ion channels - tocris bioscience · 2017-06-19 · ion channels are pore-forming proteins present...
TRANSCRIPT
Ion Channels
Products by Gating Mechanism:• Ligand-gated Ion Channels• Voltage-gated Ion Channels• Other Ion Channels
Western Honey BeeApis melliferaA source of Apamin
Product Listing | Edition 1
Tocris Product Listing Series
2 |
IntroductionIon channels are pore-forming proteins present in the plasma membrane of most cells, as well as the intracellular membranes surrounding many organelles, allowing the passage of ions across the membrane. They are essential for maintaining resting membrane potential, generating action potentials and other electrical signaling, and regulating cell volume. Ion channels have a fundamental role in physiological processes such as T cell activation, muscle contraction, insulin release from pancreatic β cells and transport of nutrients and ions across epithelial cells. A huge variety of ion channels exist, exhibiting selective permeability to particular ions and having different gating mechanisms. Ion channels may be classified according to their ion selectivity or gating mechanism, i.e. how the flow of ions is controlled. We have followed the IUPHAR classification of ion channels for the purposes of this listing and grouped the products into three main sections according to gating mechanism: Ligand-gated Ion Channels, Voltage-gated Ion Channels, and Other Channels.
Contents
Front cover image by Mikhail Laptev (https://www.dreamstime.com/royalty-free-stock-photography-honey-bee-apis-mellifera-dahlia-flower-image27164717) via dreamstime.com
Ligand-gated Ion Channels 3
5-HT3 4
AcetylcholineNicotinicReceptors 4
Nicotinic (α7) Receptors 4
Nicotinic (α4β2) Receptors 6
Nicotinic Receptors (Non-selective/Other) 7
Acid-sensingIonChannels 8
EpithelialSodiumChannels 8
GABAAandGABAA-ρReceptors 8
GABAA Receptors 8
GABAA-ρ Receptors 9
GABA Miscellaneous 9
Glutamate(Ionotropic)Receptors 9
AMPA Receptors 9
Kainate Receptors 10
NMDA Receptors 10
Other Glutamate 12
GlycineReceptors 13
HCNChannels 13
IP3Receptors 13
Purinergic(P2X)Receptors 13
Voltage-gated Ion Channels 15
CalciumChannels 16
Ryanodine Receptors 16
STIM-Orai Channels 16
Voltage-gated Calcium Channels 16
Other Calcium Channels 17
PotassiumChannels 17
Ca2+-Activated Potassium Channels 17
Inward Rectifier Potassium (Kir) Channels 18
Two-P Potassium Channels 19
Voltage-gated Potassium (Kv) Channels 19
Non-selective / Other Potassium Channels 19
SodiumChannels 20
Voltage-gated Sodium Channels 20
TransientReceptorPotentialChannels 20
TRPA1 20
TRPC 20
TRPM 20
TRPML 21
TRPP 21
TRPV 21
The Comprehensive in Vitro Proarrhythmia 23Assay Initiative (CiPA)
Other Channels 24
Aquaporins 24
ChlorideChannels 24
Calcium-activated Chloride Channels 24
CFTR 24
Other Chloride Channels 24
Ionophores 24
PhotoswitchableLigands 25
OtherChannelModulators 25
Antibodies Targeting Ion Channels 26
References 27
Ion channeLS
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GRIN1
GRIN3B
GRIN3A
GLRA3
GLRA1
GLRA2GLRA4
GLRBGABRR2
GABRR1GABRR3
GABRP
GABRD
GABRB3
GABRB2
GABRB1
GABRQ
GABRG2
GABRG1
GABRG3GABRE
GABRA6
GABRA4
GABRA2
GABRA1GABRA5GABRA3
CHRNA1
HTR3A HTR3B HTR3D
HTR3CHTR3ECHRNA2CHRNA4
CHRNA3CHRNA6
CHRNA
CHRNB3CHRNB2CHRNB4
CHRNB1CHRND
CHRNECHRNG
CHRNA7
CHRNA10
CHRNA9
GRIA3GRIA1
GRIA2
GRIA4
GRIK2
GRIK1
GRIK3GRIK4
GRIK5
GRIN2D
GRIN2C
GRIN2B
GRIN2A
P2XENaC
ASIC
NMDA
Kainate
AMPA
nAChR
5-HT
GlyR
GABAa
P2RX3
P2RX2 P2RX4
P2RX1
P2RX5
P2RX6
P2RX7
SCNN1A SCNN1D
SCNN1B
SCNN1G
ASIC2
ASIC1
ASIC3
ASIC4
ASIC5
Figure 1 | A representation of the ligand-gated ion channel gene tree featuring genes of ion channels targeted by tocris products
Ligand-gated Ion channelsLigand-gated ion channels are a large group of transmembrane proteins that allow the passage of ions through the membrane in response to the binding of a specific chemical messenger; they are also known as ionotropic receptors. Ligand-gated ion channels are grouped according to the endogenous compound to which they selectively respond; these include 5-HT, ATP, GABA, glutamate, acetylcholine and glycine. In general, the binding site for the ligand is distinct from the pore, and binding results in either channel opening or closing.
Gene abbreviation
Ion Channel
ASIC acid-sensing ion channelCHRNA cholinergic receptor nicotinic alpha subunit CHRNB cholinergic receptor nicotinic beta subunit CHRND cholinergic receptor nicotinic delta subunit CHRNE cholinergic receptor nicotinic epsilon subunit CHRNG cholinergic receptor nicotinic gamma subunit GABRA γ-aminobutyric acid type a receptor alpha subunitGABRB γ-aminobutyric acid type a receptor beta subunitGABRD γ-aminobutyric acid type a receptor delta subunitGABRE γ-aminobutyric acid type a receptor epsilon
subunitGABRG γ-aminobutyric acid type a receptor gamma
subunitGABRP γ-aminobutyric acid type a receptor pi subunitGABRQ γ-aminobutyric acid type a receptor theta subunitGABRR γ-aminobutyric acid type a receptor rho subunitGRIA glutamate ionotropic receptor aMPa type subunitGRIK glutamate ionotropic receptor kainate type
subunitGRIN glutamate ionotropic receptor nMDa type subunitGLRA glycine receptor alphaGLRB glycine receptor betaHTR3 5-hydroxytryptamine receptor 3P2RX purinergic receptor P2XSCNN sodium channel epithelial (enac)
adapted from www.guidetopharmacology.org
Tocris Product Listing Series
4 |
5-HT3
Agonists 0440 m-chlorophenylbiguanide Potent and specific 5-hT3 agonist 100 mg
0558 2-Methyl-5-hydroxytryptamine 5-hT3 agonist/potent 5-hT6 ligand 10 mg
50 mg
0566 N-Methylquipazine 5-hT3 agonist 100 mg
0629 Quipazine 5-hT3 agonist 100 mg
0988 RS 56812 5-hT3 partial agonist 10 mg
50 mg
3547 Serotonin endogenous 5-hT receptor agonist 50 mg
1205 SR 57227 Potent, selective 5-hT3 agonist 10 mg
50 mg
Antagonists 0666 3-aQc 5-hT3 antagonist 10 mg
50 mg
2759 B-hT 920 5-hT3 antagonist; also α2 agonist and D2 receptor agonist 10 mg
50 mg
0475 Dihydroergotamine non-selective 5-hT antagonist; also partial α agonist 100 mg
5629 Dolasetron Potent and selective 5-hT3 antagonist 10 mg
50 mg
2903 Granisetron 5-hT3 antagonist 10 mg
50 mg
0640 MDL 72222 5-hT3 antagonist 50 mg
2018 Mirtazapine 5-hT3, 5-hT2, h1 and α2-antagonist; antidepressant 10 mg
50 mg
2844 Mosapride citrate 5-hT3 antagonist and 5-hT4 agonist 10 mg
50 mg
2891 ondansetron Selective 5-hT3 antagonist 10 mg
50 mg
2037 SDZ 205-557 5-hT3 and 5-hT4 receptor antagonist 10 mg
50 mg
0641 Tropanyl-3,5-dimethylbenzoate 5-hT3 antagonist 100 mg
2459 Tropisetron Potent 5-hT3 receptor antagonist; also partial agonist of α7 nachR 10 mg
50 mg
4532 VUF 10166 high affinity 5-hT3 receptor antagonist 10 mg
50 mg
0380 Y-25130 Potent, selective 5-hT3 antagonist 10 mg
50 mg
1795 Zacopride highly potent 5-hT3 receptor antagonist; also 5-hT4 agonist 10 mg
50 mg
AcetylcholineNicotinicReceptorsnicotinic (α7) Receptors
Agonists 4234 4BP-TQS allosteric agonist at α7 nachR 10 mg
4341 a 582941 Partial agonist at α7 nachR 10 mg
50 mg
4477 a 844606 Selective α7 nachR partial agonist 10 mg
50 mg
2809 acetylcholine endogenous neurotransmitter 50 mg
3964 aR-R 17779 α7-selective agonist 10 mg
2241 DMaB-anabaseine Partial agonist at α7 nachR; also α4β2 antagonist 10 mg
50 mg
4557 GTS 21 Partial agonist at α7 nachR 10 mg
50 mg
3092 Pha 543613 Potent and selective α7 nachR agonist 10 mg
3134 Pha 568487 α7-selective agonist 10 mg
50 mg
2303 PnU 282987 Selective α7 nachR agonist 10 mg
50 mg
Category Cat. no. Product name Description Unit size
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1271 RJR 2429 nicotinic receptor agonist 10 mg
50 mg
3518 S 24795 Partial agonist at α7 nachR 10 mg
50 mg
4441 Sen 12333 α7 nachR agonist; histamine h3 antagonist 10 mg
50 mg
5559 SSR 180711 Partial agonist at α7 nachR 10 mg
50 mg
2518 Tc 1698 α7-selective agonist 10 mg
50 mg
Antagonists 2133 α-Bungarotoxin α7 subtype-selective nachR antagonist 1 mg
3119 α-conotoxin ImI α7 and α9 selective nachR antagonist 500 μg
3405 coG 133 nicotinic α7 antagonist; apoe peptide fragment 1 mg
1029 Methyllycaconitine α7 neuronal nicotinic receptor antagonist 5 mg
25 mg
1356 MG 624 α7 neuronal nicotinic receptor antagonist 10 mg
50 mg
Modulators 4571 a 867744 Positive allosteric modulator of α7 nachR 10 mg
50 mg
3837 ccMI Positive allosteric modulator of α7 nachR 10 mg
50 mg
1260 Ivermectin allosteric modulator of α7 nicotinic receptors 100 mg
Ligand-gated Ion channels – continued
Immunology feature products
NN
N
N Cl
Cl
N
A 438079 (2972)Competitive P2X7 receptor antagonist
HNO
HN
OHN
O
HN
O
HN
SO3Na
SO3Na
NaO3S
NaO3S
NaO3S
NaO3S
OHN
NaO3S
NaO3S
NF 449 (1391)Potent and selective P2X1
receptor antagonist
NN
Cl
TRAM 34 (2946)Potent and highly selective KCa3.1
channel blocker
O
OMeN
N
OMe
SKF 96365 (1147)Inhibits STIM1-mediated Ca2+
influx; also TRPC channel inhibitor
OH
NH
NH
SO
O
5J 4 (5490)CRAC channel blocker; blocks store-operated calcium entry
P2X7 receptors expressed on T cells and microglia are associated with cell migration, proliferation, and cytokine release as well as
Th17 differentiation.Calcium is a second messenger in
lymphocytes, regulating proliferation, gene expression, motility and other functions. STIM1 is the putative Ca2+ sensor on the
endoplasmic reticulum (ER).
Potassium channels regulate the membrane potential of lymphocytes and KCa3.1
channels are associated with membrane hyperpolarization in response to elevated
intracellular Ca2+ levels.
CRAC channels are expressed in lymphocytes and are activated in response
to depleted intracellular Ca2+ stores. Ca2+ release from ER is triggered by IP3 in response to antigen receptor activation.
P2X1 receptors are expressed on T cells and are associated activation.
Ion Channels in Immunology Research T and B cells and microglia express a wide variety of ion channels, which are implicated in immune processes. Below is a selection of compounds from Tocris that may be used to explore the role of ion channels in the immune system.
Category Cat. no. Product name Description Unit size
Tocris Product Listing Series
6 |
4141 LY 2087101 Potentiator of α7 nachRs 10 mg
50 mg
2995 nS 1738 Positive allosteric modulator of α7 nachR; active in vivo 10 mg
50 mg
2498 PnU 120596 Positive allosteric modulator of α7 nachR; active in vivo 10 mg
50 mg
4233 TQS Positive allosteric modulator of α7 nachRs 10 mg
50 mg
Other 5156 Ivermectin B1a-d2 Deuterated ivermectin B1a (cat. no. 1260) 1 mg
nicotinic (α4β2) receptors
Agonists 5017 a 85380 high affinity and selective α4β2 agonist 10 mg
5079 aBT 089 high affinity and selective α4β2 partial agonist 10 mg
50 mg
5236 cc4 high affinity and subtype-selective α6β2 and α4β2 partial agonist 10 mg
50 mg
4125 3-pyr-cytisine high affinity, partial agonist of α4β2 receptors 10 mg
50 mg
5557 Dianicline Selective α4β2 nachR partial agonist 10 mg
50 mg
1518 5-Iodo-a-85380 high affinity α4β2 and α6β2 subtype-selective agonist 10 mg
1527 5-Iodo-a-85380, 5-trimethylstannyl n-Boc derivative
Precursor to 5-Iodo-a-85380 (cat. no. 1518) 200 μg
1053 RJR 2403 α4β2 selective nicotinic agonist 10 mg
50 mg
2737 Tc 2559 Selective partial agonist at α4β2 receptors 10 mg
50 mg
3754 Varenicline orally active, subtype-selective α4β2 partial agonist 10 mg
50 mg
2nd agonist/competitive antagonist site
Agonist/competitive antagonist binding siteat subunit interface
M2 lines the cation channel
Subunit topographyPentameric nAChR with central cation channel and notional sites for drug interactions
Allosteric modulator sites
Channel blocker/non-competitive antagonist
Ca2+, Na+
K+
Out
In
M1 M2 M3 M4
C
N
Cys-loop
ACh binding protein (AChBP)
CC
Category Cat. no. Product name Description Unit size
Left: The topography of a single nachR subunit. The two cysteine residues forming the signature cys-loop are indicated. The extracellular n-terminal domain corresponds to the achBP. Right: Schematic of a generic nachR showing 5 subunits spanning the membrane to form a central ion channel. notional sites of action of interacting drugs are shown: two agonist binding sites are indicated at extracellular subunit interfaces, consistent with a heteromeric nachR. competitive antagonist sites overlap the agonist binding sites. extracellular and intramembrane sites have been proposed for different allosteric modulators. non-competitive antagonists may occlude or block the ion channel, as indicated, or may act at other sites. See text for further details.
Ion channeLS
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Modulators 3328 Desformylflustrabromine Positive allosteric modulator of α4β2; also muscle-type nachR inhibitor
10 mg
50 mg
5112 nS 9283 Positive allosteric modulator of α4β2 10 mg
50 mg
Other 2736 Sazetidine a α4β2 receptor ligand; may act as an agonist or a desensitizer 10 mg
nicotinic Receptors (non-selective/other)
Agonists 0351 1-acetyl-4-methylpiperazine nicotinic agonist 10 mg
50 mg
0352 4-acetyl-1,1-dimethylpiperazinium nicotinic agonist 10 mg
50 mg
1971 (+)-anabasine neuronal nicotinic receptor partial agonist 50 mg
0789 (±)-anatoxin a nicotinic agonist 1 mg
3549 3-Bromocytisine Potent agonist of α4β4, α4β2 and α7 nach receptors 10 mg
50 mg
2810 carbamoylcholine cholinergic receptor agonist 100 mg
3110 (-)-cotinine Major metabolite of nicotine 50 mg
1390 (-)-cytisine Potent, selective neuronal nicotinic agonist 10 mg
50 mg
0684 (±)-epibatidine high affinity nicotinic agonist 10 mg
1077 (-)-Lobeline nicotinic partial agonist 100 mg
3546 (-)-nicotine Prototypical nachR agonist 50 mg
4831 nS 3861 α3β2 full agonist; also α3β4 partial agonist 10 mg
50 mg
3855 RuBi-nicotine caged nicotine; rapidly excitable by visible light 10 mg
4766 SIB 1508Y Potent agonist of α4β2, α2β4, α4β4 and α3β4 nach receptors 10 mg
50 mg
4764 SIB 1553a Subunit selective nachR agonist 10 mg
50 mg
1348 UB 165 Subunit selective nachR agonist 10 mg
Antagonists 3205 acV 1 α9α10-selective antagonist 100 μg
4128 Bisindolylmaleimide II nicotinic receptor antagonist; also potent PKc inhibitor 10 mg
50 mg
Ligand-gated Ion channels – continued
Human α4β2 nicotinic ReceptorX-Ray crystal structure of α4β2 nicotinic receptor in complex with nicotine
Image adapted from RScB Protein Data Bank (http://www.rcsb.org). PDB ID: 5KXI Morales-Perez et al. (2016) Nature 538 411. PMID 27698419.
• Nicotine is the prototypical nAChR agonist (Ki = 1 nM)
• The effects of nicotine in the brain, including its reinforcing properties that lead to addiction, are mediated by α4β2 receptors
• Nicotine binds in the classical neurotransmitter site at the α–β interface.
Cat. No. 3546N
N
Cat. No. 3546
Cat. No. 2555O
MeHN
.HCI
O
ON
N
O
Category Cat. no. Product name Description Unit size
Tocris Product Listing Series
8 |
0424 Benzoquinonium nicotinic antagonist 10 mg
50 mg
3221 bPiDDB orthosteric nachR antagonist 10 mg
50 mg
2722 catestatin non-competitive nicotinic cholinergic antagonist 1 mg
1001 chlorisondamine nicotinic antagonist; slow offset 10 mg
50 mg
3120 α-conotoxin auIB Selective α3β4 nachR antagonist 500 μg
3124 α-conotoxin eI α1β1δγ selective nachR antagonist 500 μg
1340 α-conotoxin MII Potent α3β2 and β3 subunit selective nicotinic antagonist 500 μg
3121 α-conotoxin PIa Selective antagonist of α6-containing nicotinic receptors 500 μg
3123 α-conotoxin PnIa Selective α3β2 nachR antagonist 500 μg
2349 Dihydro-β-erythroidine antagonist for neuronal α4-containing nicotinic receptors 10 mg
50 mg
4111 hexamethonium nicotinic receptor blocker 50 mg
2843 Mecamylamine non-competitive nicotinic receptor antagonist 10 mg
50 mg
0693 Pancuronium nicotinic (neuromuscular) antagonist 10 mg
50 mg
4424 SR 16584 Selective α3β4 nachR antagonist 10 mg
50 mg
2438 TMPh neuronal nicotinic receptor antagonist 10 mg
50 mg
2820 (+)-Tubocurarine nicotinic receptor antagonist 50 mg
Other 0686 Galanthamine neuronal nicotinic receptor potentiator; also cholinesterase inhibitor 100 mg
Acid-SensingIonChannelsActivators 5028 GMQ Selective aSIc3 opener 10 mg
50 mg
Blockers 4804 aPeTx2 aSIc3 channel blocker 100 μg
5938 Mambalgin 1 Selective aSIc1a inhibitor; analgesic 10 μg
5042 Psalmotoxin 1 Potent and selective aSIc1a channel blocker 100 μg
EpithelialSodiumChannelsActivators 0464 capsazepine activator of enacδ; also vanilloid receptor antagonist 10 mg
50 mg
Blockers 3380 Benzamil Deg/enac channel blocker; amiloride (cat. no. 0890) derivative; also ncX inhibitor
10 mg
50 mg
GABAAandGABAA-ρReceptorsGABAA Receptors
Agonists 0289 Muscimol Potent GaBaa agonist 1 mg
10 mg
50 mg
0807 ThIP GaBaa agonist; also GaBaa -ρ antagonist 50 mg
Antagonists 2503 (-)-Bicuculline methiodide Water-soluble GaBaa antagonist 10 mg
50 mg
0109 (-)-Bicuculline methobromide Water-soluble GaBaa antagonist 10 mg
50 mg
0131 (-)-Bicuculline methochloride Water-soluble GaBaa antagonist 10 mg
50 mg
0130 (+)-Bicuculline Potent GaBaa antagonist 50 mg
1128 Picrotoxin GaBaa receptor antagonist 1 g
1262 SR 95531 Selective, competitive GaBaa receptor antagonist 10 mg
50 mg
Benzodiazepines 5281 ac 5216 Selective TSPo ligand 10 mg
50 mg
1327 L-655,708 Benzodiazepine inverse agonist; selective for α5-containing GaBaa receptors
10 mg
50 mg
Category Cat. no. Product name Description Unit size
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2832 Midazolam Benzodiazepine agonist 10 mg
50 mg
0670 PK 11195 antagonist at peripheral benzodiazepine receptors 10 mg
50 mg
0655 Zolpidem Benzodiazepine agonist 10 mg
50 mg
Modulators 3653 allopregnanolone GaBaa receptor positive allosteric modulator 10 mg
3113 etifoxine Potentiator of GaBaa receptors; anxiolytic 10 mg
50 mg
1471 etomidate GaBa mimetic and GaBa modulatory agent 10 mg
50 mg
2531 Ganaxolone Potent, positive allosteric modulator of GaBaa receptors 10 mg
50 mg
3652 Pregnanolone GaBaa receptor positive allosteric modulator 50 mg
GABAA-ρ Receptors
Agonists 0379 SKF 97541 GaBaa-ρ antagonist; also extremely potent GaBaB agonist 10 mg
50 mg
0180 ZaPa agonist at ‘low affinity’ GaBaa receptor; more potent than GaBa/muscimol
10 mg
50 mg
Antagonists 1040 TPMPa Selective GaBaa-ρ antagonist 10 mg
50 mg
GABA Miscellaneous
Other 2991 DPnI-caged-GaBa nitroindoline-caged GaBa 10 mg
2687 Pentylenetetrazole convulsant 1 g
3400 RuBi-GaBa caged GaBa; excitable by visible wavelength 10 mg
Glutamate(Ionotropic)ReceptorsAMPA Receptors
Antagonists 2555 GYKI 53655 non-competitive aMPa receptor antagonist 10 mg
50 mg
1636 IeM 1460 open-channel blocker of aMPa currents; selective for non-GluR2-containing receptors
10 mg
50 mg
2345 ZK 200775 competitive aMPa/kainate antagonist 10 mg
50 mg
Ligand-gated Ion channels – continued
AMPA-subtype Ionotropic Glutamate ReceptorX-Ray crystal structure of rat GluA2 receptor in complex with the noncompetitive inhibitor GYKI 53655
Image adapted from RScB Protein Data Bank (http://www.rcsb.org). PDB ID: 5L1h Yelshanskaya et al. (2016) Neuron 91 1305. PMID 27618672
• GYKI 53655 is a non-competitive AMPA and kainate receptor antagonist. IC50 is 18.9 μM for AMPA receptors.
• GYKI 53655 exhibits anticonvulsant activity.
• The compound binds at the interface between the ion channel and the linkers connecting the transmembrane domain and the ligand-binding domain.
Cat. No. 2555
N
N
Cat. No. 3546
Cat. No. 2555O
MeHN
.HCI
O
ON
N
O
Category Cat. no. Product name Description Unit size
Tocris Product Listing Series
10 |
Other 6094 2R,6R-hydroxynorketamine enhances aMPa currents; metabolite of Ketamine (cat. no. 3131) 10 mg
6095 2S,6S-hydroxynorketamine enhances aMPa currents; metabolite of Ketamine (cat. no. 3131) 10 mg
5982 cis-6-hydroxynorketamine enhances aMPa currents; metabolite of Ketamine (cat. no. 3131) 10 mg
50 mg
Kainate Receptors
Agonists 0269 Domoic acid Potent, selective kainate agonist 1 mg
5 mg
0222 Kainic acid Potent excitant and neurotoxin 1 mg
10 mg
50 mg
Antagonists 2728 aceT Potent antagonist of GluR5-containing kainate receptors 10 mg
0190 cnQX Potent aMPa/kainate antagonist 10 mg
50 mg
1045 cnQX disodium salt Potent aMPa/kainate antagonist; more water soluble form of cnQX (cat. no. 0190)
1 mg
10 mg
50 mg
0189 DnQX Selective non-nMDa antagonist 10 mg
50 mg
2312 DnQX disodium salt Selective non-nMDa antagonist; water-soluble salt of DnQX (cat. no. 0189)
10 mg
50 mg
3620 Topiramate GluR5 antagonist; inhibits carbonic anhydrase (ca) II and IV 10 mg
50 mg
2079 UBP 302 Potent and selective kainate antagonist; active enantiomer of UBP 296 (cat. no. 2078)
10 mg
50 mg
nMDA Receptors
Agonists 0186 cis-acPD Potent nMDa agonist; also group II mGluR agonist 10 mg
50 mg
0213 d-aspartic acid nMDa agonist 1 g
0214 l-aspartic acid nMDa agonist 1 g
0216 l-cysteinesulfinic acid nMDa and mGlu agonist 100 mg
3406 GLYX 13 nMDa receptor partial agonist; acts at the glycine site 1 mg
0197 homoquinolinic acid Selective, potent nMDa agonist 10 mg
50 mg
0285 Ibotenic acid non-selective nMDa agonist 5 mg
2277 MnI-caged-d-aspartate caged d-aspartate; nMDa agonist 10 mg
50 mg
0114 nMDa Selective nMDa agonist 50 mg
500 mg
0225 Quinolinic acid endogenous nMDa agonist and transmitter candidate 1 g
0959 Spermidine tri agonist at polyamine site of nMDa receptor 100 mg
0312 (RS)-(Tetrazol-5-yl)glycine highly potent nMDa receptor agonist 10 mg
50 mg
Antagonists 0106 d-aP5 Potent, selective nMDa antagonist; more active form of dl-aP5 (cat. no. 0105)
1 mg
10 mg
50 mg
100 mg
0105 dl-aP5 Potent, selective nMDa antagonist 10 mg
50 mg
3693 dl-aP5 sodium salt nMDa antagonist; sodium salt of dl-aP5 (cat. no. 0105) 10 mg
50 mg
0104 dl-aP7 Selective nMDa antagonist 10 mg
50 mg
0107 l-aP5 Potent, selective nMDa antagonist; less active form of dl-aP5 (cat. no. 0105)
10 mg
50 mg
1469 cGP 37849 Potent and selective nMDa antagonist 10 mg
50 mg
Category Cat. no. Product name Description Unit size
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1409 cGP 39551 Potent, selective and competitive nMDa antagonist 10 mg
50 mg
1493 cGP 78608 Potent, selective glycine-site nMDa antagonist 10 mg
50 mg
1241 cGS 19755 Potent, competitive nMDa antagonist 10 mg
50 mg
0237 7-chlorokynurenic acid nMDa receptor antagonist; also potent competitive inhibitor of l-glutamate uptake
10 mg
50 mg
3697 7-chlorokynurenic acid sodium salt nMDa antagonist; also potent competitive inhibitor of L-glutamate uptake; sodium salt of 7-chlorokynurenic acid (cat. no. 0237)
10 mg
50 mg
2456 co 101244 highly selective nR2B antagonist 10 mg
50 mg
4136 conantokin G nR2B-selective nMDa receptor antagonist 500 μg
3125 conantokin-R Potent non-competitive nMDa receptor antagonist 500 μg
3122 conantokin-T non-competitive nMDa receptor antagonist 500 μg
0247 (R)-cPP Potent nMDa antagonist; more active enantiomer of (RS)-cPP (cat. no. 0173)
10 mg
50 mg
0173 (RS)-cPP Potent nMDa antagonist 10 mg
50 mg
1265 d-cPP-ene Potent, competitive nMDa antagonist 10 mg
0286 5,7-Dichlorokynurenic acid Potent nMDa antagonist, acts at glycine site 10 mg
50 mg
3698 5,7-Dichlorokynurenic acid sodium salt Potent nMDa antagonist, acts at glycine site; sodium salt of 5,7-Dichlorokynurenic acid (cat. no. 0286);
10 mg
50 mg
0360 (±)-1-(1,2-Diphenylethyl)piperidine nMDa antagonist, acts at ion channel site 10 mg
50 mg
4491 DQP 1105 Selective nR2c/nR2D receptor antagonist 10 mg
50 mg
2195 eliprodil non-competitive nR2B-selective nMDa antagonist 10 mg
50 mg
2348 Gavestinel Potent and selective glycine site antagonist; orally available and active in vivo
10 mg
50 mg
0545 Ifenprodil non-competitive nMDa antagonist; also σ ligand 10 mg
50 mg
3131 Ketamine non-competitive nMDa receptor antagonist 50 mg
4379 (S)-(+)-Ketamine nMDa receptor antagonist; enantiomer of ketamine (cat. no. 3131) 50 mg
0742 L-689,560 Very potent nMDa antagonist 10 mg
50 mg
1019 LY 235959 competitive nMDa antagonist 10 mg
50 mg
0773 Memantine nMDa antagonist; acts at ion channel site 50 mg
0924 (+)-MK 801 maleate non-competitive nMDa antagonist; acts at ion channel site 10 mg
50 mg
0955 (-)-MK 801 maleate nMDa antagonist, less active enantiomer 10 mg
50 mg
1970 norketamine Potent, non-competitive nMDa antagonist 10 mg
50 mg
5018 PeaQX tetrasodium salt Potent nMDa receptor antagonist; nR2a selective 10 mg
2557 Phencyclidine non-competitive nMDa receptor antagonist 10 mg
50 mg
2530 PPDa Subtype-selective nR2c/nR2D antagonist 10 mg
50 mg
2274 PPPa competitive nR2a antagonist 10 mg
50 mg
4801 QnZ 46 nR2c/nR2D-selective nMDa receptor non-competitive antagonist 10 mg
50 mg
Ligand-gated Ion channels – continued
Category Cat. no. Product name Description Unit size
Tocris Product Listing Series
12 |
2005 Ro 04-5595 nR2B-selective nMDa antagonist 10 mg
50 mg
1594 Ro 25-6981 nR2B-selective nMDa antagonist 1 mg
10 mg
50 mg
3343 Ro 8-4304 nR2B-selective nMDa antagonist 10 mg
50 mg
1250 SDZ 220-581 competitive nMDa antagonist 10 mg
50 mg
4154 Tcn 201 Selective nR1/nR2a receptor antagonist 10 mg
50 mg
4163 Tcn 213 nMDa antagonist; selective for nR2a over nR2B 10 mg
50 mg
4072 Tcn 237 highly potent and selective nR2B antagonist 10 mg
2782 TcS 46b orally active, subtype-selective nR1a/nR2B antagonist 10 mg
50 mg
2892 Threo Ifenprodil nR2B-selective nMDa antagonist; also σ agonist 10 mg
50 mg
3322 ZD 9379 Brain penetrant nMDa antagonist; acts at glycine site 10 mg
Other 4105 cIQ Potentiator of nMDa receptors containing nR2c/nR2D 10 mg
50 mg
0226 d-Serine nMDa potentiator; acts at glycine site 1 g
2224 MnI-caged-nMDa caged nMDa 10 mg
2213 n20c non-competitive nMDa receptor open-channel blocker 10 mg
50 mg
5996 R-norketamine nMDa receptor modulator; metabolite of Ketamine (cat. no. 3131) 10 mg
6112 S-norketamine nMDa receptor modulator; metabolite of Ketamine (cat. no. 3131) 10 mg
4230 nPec-caged-d-aP5 caged d-aP5 (cat.no. 0106) 10 mg
50 mg
5376 Pregnenolone sulfate sodium salt nMDa Potentiator 50 mg
0958 Spermine Modulator at polyamine site on nMDa receptors 100 mg
other Glutamate
Agonists 0217 d-Glutamic acid endogenous, non-selective agonist; less active enantiomer 1 g
0218 l-Glutamic acid endogenous, non-selective agonist 1 g
0391 Spaglumic acid Weak activator of nMDa receptors; also selective mGlu3 agonist 50 mg
Antagonists 0102 d-aP4 Broad spectrum eaa antagonist 10 mg
50 mg
0101 dl-aP4 Broad spectrum eaa antagonist 100 mg
3699 dl-aP4 Sodium salt Broad spectrum eaa antagonist; sodium salt of DL-aP4 (cat. no. 0101)
50 mg
0341 l-aP6 Selective agonist of the ‘quis’ effect 10 mg
50 mg
2538 l-BMaa neurotoxic amino acid 10 mg
0321 (RS)-4-carboxyphenylglycine Broad spectrum eaa ligand 10 mg
50 mg
0310 (RS)-4-carboxy-3-hydroxyphenylglycine Broad spectrum eaa ligand 10 mg
50 mg
0328 (R)-3-carboxy-4-hydroxyphenylglycine Ionotropic glutamate receptor antagonist 10 mg
50 mg
1395 (R)-3,4-DcPG aMPa antagonist; weak nMDa antagonist 10 mg
50 mg
1394 (RS)-3,4-DcPG Potent systemically active anticonvulsant. Racemate of (R)-3,4,-DcPG (cat. no. 1395)
10 mg
50 mg
0112 γDGG Broad spectrum glutamate receptor antagonist 50 mg
0223 Kynurenic acid Broad spectrum eaa antagonist 1 g
3694 Kynurenic acid sodium salt Sodium salt of kynurenic acid (cat. no. 0223) 100 mg
Category Cat. no. Product name Description Unit size
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Other 5785 MDnI-caged-l-glutamate Stable photoreleaser of l-glutamate 10 mg
1490 MnI-caged-l-glutamate Stable photoreleaser of l-glutamate 10 mg
50 mg
0395 n-acetylglycyl-d-glutamic acid Potent convulsant 10 mg
50 mg
3574 RuBi-Glutamate caged glutamate; excited by visible wavelengths 10 mg
0636 Salsolinol-1-carboxylic acid endogenous amino acid 10 mg
50 mg
3847 Theanine Glutamate receptor ligand 50 mg
GlycineReceptorsAgonists 0206 β-alanine endogenous glycine agonist; more selective than taurine
(cat. no. 0209)1 g
0205 L-alanine Glycine receptor agonist 1 g
0219 Glycine endogenous glycine agonist; also modulates nMDa receptor-mediated neurotransmission
1 g
0208 hypotaurine non-selective endogenous glycine receptor agonist 100 mg
0227 L-Serine Weak endogenous glycine receptor agonist 1 g
0209 Taurine non-selective, endogenous glycine receptor partial agonist 1 g
HCNChannelsBlockers 2202 Zatebradine Blocks hyperpolarization-activated current (If) 10 mg
50 mg
1000 ZD 7288 Inhibits pacemaker (If) current 10 mg
50 mg
IP3ReceptorsAntagonists 1224 2-aPB IP3 receptor antagonist; also TRP channel modulator 10 mg
50 mg
1280 (-)-Xestospongin c Reported inhibitor of IP3-dependent ca2+ release 10 μg
Other 6210 ci-IP3/PM caged inositol triphosphate 10 μg
Purinergic(P2X)ReceptorsAgonists 3245 aTP P2 agonist 50 mg
4080 aTPγS P2 agonist; aTP (cat. no. 3245) analog 10 mg
3312 BzaTP P2X7 agonist and P2X1/P2Y1 partial agonist; also photoaffinity label for aTPase
1 mg
3209 α,β-Methyleneadenosine 5’-triphosphate P2 agonist 10 mg
1062 2-Methylthioadenosine triphosphate P2 purinergic agonist 10 mg
Antagonists 2972 a 438079 competitive P2X7 antagonist 10 mg
50 mg
3701 a 740003 Potent and selective P2X7 antagonist 10 mg
50 mg
4473 a 804598 Potent and selective P2X7 antagonist 10 mg
50 mg
4232 a 839977 Potent P2X7 antagonist 10 mg
50 mg
3323 aZ 10606120 Potent P2X7 receptor antagonist 10 mg
50 mg
3317 aZ 11645373 Potent and selective human P2X7 antagonist 10 mg
50 mg
3579 5-BDBD Potent P2X4 receptor antagonist 10 mg
50 mg
5545 BX 430 Selective P2X4 allosteric antagonist 10 mg
50 mg
0845 evans Blue Selective P2X purinergic antagonist; also potent inhibitor of l-glutamate uptake into synaptic vesicles
1 g
0683 iso-PPaDS P2X antagonist 10 mg
50 mg
5299 JnJ 47965567 Potent and selective P2X7 antagonist; brain penetrant 10 mg
50 mg
Ligand-gated Ion channels – continued
Category Cat. no. Product name Description Unit size
Tocris Product Listing Series
14 |
1277 Kn-62 non-competitive P2X7 antagonist 1 mg
1240 nF 023 Selective, competitive P2X1 antagonist 10 mg
50 mg
2548 nF 110 Potent P2X3 antagonist 10 mg
50 mg
2450 nF 157 Selective P2Y11/P2X1 antagonist 10 mg
50 mg
1199 nF 279 Potent and selective P2X1 antagonist 10 mg
50 mg
1391 nF 449 highly selective P2X1 antagonist 10 mg
50 mg
0625 PPaDS P2 purinergic antagonist 10 mg
50 mg
1309 PPnDS Potent, selective P2X1 antagonist 10 mg
50 mg
2188 Ro 0437626 Selective P2X1 antagonist 1 mg
10 mg
4391 Ro 51 Potent P2X3, P2X2/3 antagonist 10 mg
50 mg
3052 Ro-3 Selective P2X3 and P2X2/3 antagonist 10 mg
4386 Tc-P 262 Selective P2X3, P2X2/3 antagonist 10 mg
50 mg
2464 TnP-aTP Potent, selective P2X antagonist 5 mg
Modulators 3385 GW 791343 P2X7 allosteric modulator 10 mg
50 mg
Other 5157 DMnPe-caged aTP caged aTP 10 mg
1203 MRS 2219 Potentiates P2X1-mediated responses 10 mg
50 mg
Ligand-gated Ion channels – continued
Category Cat. no. Product name Description Unit size
New Compound Libraries
Tocris has launched a range of new compound libraries composed of biologically active molecules that have proven pharmacological activity against a wide range of targets. Use them in your phenotypic screening studies, drug repurposing campaigns or for validation of new molecular targets. compounds are supplied pre-dissolved in DMSo, and full chemical and biological data are available. all compounds have the same proven solubility, purity and stability as all those in the Tocris catalog.
Tocriscreen Plus (Cat. No. 5840)A unique library of 1280 biologically active compounds, including 177 ion channel modulators, with many exclusive to Tocris (250 mL 10 mM DMSO solutions). The collection is also available in smaller aliquots of 50 μL as the Tocriscreen Plus Mini (Cat No. 5841).
Tocriscreen Library of FDA Approved Compounds (Cat. No. 5932) A library of 160 FDA-approved compounds (250 mL 10 mM DMSO solutions)
Tocris also has a Custom Compound Library service available.
For more information visit www.tocris.com/tocriscreen
Ion channeLS
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Voltage-gated Ion channelsVoltage-gated ion channels are a group of transmembrane proteins that are activated by changes in membrane potential. The alteration in membrane potential induces a conformational change in the channel protein that either opens or closes the pore. Voltage-gated ion channels are important in excitable cells such as neurons and myocytes, and they are classified according to ion selectivity, including Na+, K+, Ca2+. Also included in this group are a number of ion channel types that are relatively insensitive to changes in voltage, and are gated by second messengers or other intracellular or extracellular mediators, these include TRP channels and ryanodine receptors.
SCN11A
CACNA1G
CACNA1HCACNA1I
CACNA1ECACNA1A
CACNA1B
CACNA1C
CACNA1S
CACNA1D
CACNA1F
SCN10ASCN5A
SCN4ASCN8A
SCN9A
SCN2A
SCN3ASCN1A
TRPP3
TRPP1
TRPP2
ITPR2
ITPR1
ITPR3
TRPA1 TRPV3
TRPV4
TRPV1
TRPV2TRPV5
TRPV6MCOLN1
MCOLN2
MCOLN3
TRPC1
TRPC4
TRPC2
TRPC5
TRPC7TRPC3
TRPM1
TRPM3TRPM6TRPM7
TRPM
TRPC
TRPML
K2P
TRPV
IP3
TRPP
Kir
KCa
Kv4
Kv7
Kv6
Kv9
Kv2
Kv8
Kv5
Kv3
Kv1
HCN
Kv10
ORAI
Kv11Kv12
NaV
CaV
TRPA
TRPM2
TRPM8
TRPC6
TRPM4
TRPM5
ORAI1
ORAI2
ORAI3
HCN1HCN2
KCNH1
KCNH5
KCNH7
KCNH2
KCNH6KCNH8
KCNH4
KCNH3
RYR1
RYR2
RYR3
KCNG1KCNG2
KCNG3KCNG4
KCNS3
KCNK7KCNK6
KCNK1
KCNK4
KCNK2
KCNK10KCNK5
KCNK3
KCNK9
KCNK12 KCNK13
KCNK18 KCNK18
KCNK18
KCNN4KCNN3
KCNN2
KCNU1
KCNJ15
KCNJ10KCNJ1
KCNJ8
KCNJ11KCNJ2
KCNJ12KCNJ4
KCNJ14KCNJ6
KCNJ5
KCNJ9
KCNJ3
KCNJ16
KCNJ13
KCNN1
KCNMA1KCNK16
KCNS2KCNS1
KCNB2
KCNB1
KCNV1KCNV2 KCNF1
KCNC3
KCNC4KCNC1 KCNC2
KCNA10KCNA5
KCNA6KCNA2
KCNA7KCNA1
KCNA3
KCNA4
KCND3
KCND2
KCND1
KCNQ1KCNQ2
KCNQ3KCNQ4
KCNQ5
HCN3
HCN4
Figure 2 | A representation of the voltage-gated ion channel gene tree featuring genes of ion channels targeted by tocris products
Gene abbreviation
Ion Channel
CACNA calcium voltage-gated channel subunits (caV)HCN hyperpolarization-activated cyclic nucleotide gated
potassium channelITPR IP3 receptorKCNA potassium voltage-gated channel subfamily a (Kv1)KCNB potassium voltage-gated channel subfamily B (Kv2)KCNC potassium voltage-gated channel subfamily c (Kv3)KCND potassium voltage-gated channel subfamily D (Kv4)KCNF potassium voltage-gated channel subfamily F (Kv5)KCNG potassium voltage-gated channel subfamily G (Kv6)KCNH potassium voltage-gated channel subfamily h
(Kv10, Kv11 and Kv12)KCNJ potassium voltage-gated channel subfamily J (Kir)KCNK two-pore potassium channel family (K2P)KCNMA1 potassium calcium-activated channel subfamily
M alpha 1 (Kca1.1)KCNN potassium calcium-activated channel subfamily nKCNQ potassium voltage-gated channel subfamily Q (Kv7)KCNS potassium voltage-gated channel subfamily S (Kv9)KCNU potassium calcium-activated channel subfamily U
(Kca5.1)KCNV potassium voltage-gated channel subfamily V (Kv8)
MCOLN transient receptor potential mucolipin familyORAI oRaI calcium release-activated calcium modulators RYR ryanodine receptorSCNA sodium voltage-gated channel alpha subunits (naV)TRPA transient receptor potential ankyrin family
TRPC transient receptor potential canonical familyTRPM transient receptor potential melastatin familyTRPP transient receptor potential (polycystin)/polycystic
kidney disease 2 familyTRPV transient receptor potential vanilloid family
adapted from www.guidetopharmacology.org
Tocris Product Listing Series
16 |
CalciumChannelsRyanodine Receptors
Activators 2793 caffeine Mobilizes calcium from intracellular stores; also a1 and a2B antagonist and cnS stimulant
100 mg
3905 naaDP RYR1 activator; ca2+ mobilizing agent 10 mg
1472 Suramin hexasodium salt Increases RYR open probability; also non-selective P2 antagonist 100 mg
Inhibitors 0507 Dantrolene Ryanodine receptor inhibitor; ca2+ release inhibitor 100 mg
4564 JTV 519 Ryanodine receptor (RyR) inhibitor 10 mg
50 mg
1329 Ryanodine ca2+ release inhibitor 1 mg
stIM-orai Channels
Inhibitors 5490 5J 4 cRac channel blocker; anti-inflammatory 10 mg
50 mg
0431 ML 9 STIM1-plasma membrane interaction inhibitor; also myosin light chain kinase inhibitor
10 mg
50 mg
1866 MRS 1845 Potent Soce inhibitor; blocks capacitative ca2+ entry 10 mg
50 mg
1147 SKF 96365 Inhibits store-operated ca2+ entry; also TRPc channel blocker 10 mg
50 mg
3939 YM 58483 Inhibitor of Soce in non-excitable cells 10 mg
50 mg
Voltage-gated Calcium Channels
Activators 1544 (±)-Bay K 8644 ca2+ channel activator (L-type) 10 mg
50 mg
1546 (S)-(-)-Bay K 8644 ca2+ channel activator (L-type) 10 mg
50 mg
1403 FPL 64176 Potent activator of ca2+ channels (L-type) 10 mg
50 mg
Cancer feature products
N N Me
O
HN
SMe
O O
E 4031 (1808)KV11.1 (hERG) channel blocker
Thr-Ile-Ile-Asn-Val-Lys-Cys-Thr-Ser-Pro-
Lys-Gln-Cys-Leu-Pro-Pro-Cys-Lys-Ala-Gln-
Phe-Gly-Gln-Ser-Ala-Gly-Ala-Lys-Cys-Met-
Asn-Gly-Lys-Cys-Lys-Cys-Tyr-Pro-His
Margatoxin (3563)Potent KV1.3 channel blocker
OO
NO
O
O OO
O
N
O O O
O
O O
O
O
O
O
BAPTA AM (2787)Blocks hKV1.5, hKV11.1 (hERG)
and hKV1.3 channels; also cell-permeable calcium chelator
N NHN
CF3
F3CO
S N
N
YM 58483 (3939)Store-operated Ca2+ entry (SOCE) blocker
in non-excitable cells; inhibits calcium release-activated calcium (CRAC) channels
Ion Channels in Cancer ResearchIon channels have recently emerged as playing a key role in the pathophysiology of cancer. Ion channels are present in all cancers and are involved in tumor development, proliferation, progression and invasiveness. For a comprehensive review of the role of ion channels in cancer see: Djamgoz et al. (2014) Philos.Trans.R.Soc.B.Biol.Sci. 369 (theme issue). Below is a selection of Tocris compounds that may be of use for exploring the role of ion channels in cancer.
Category Cat. no. Product name Description Unit size
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Blockers 2799 ω-agatoxin IVa ca2+ channel blocker (P-type) 10 μg
2802 ω-agatoxin TK ca2+ channel blocker (P/Q-type) 10 μg
1085 ω-conotoxin GVIa ca2+ channel blocker (n-type) 250 μg
1084 ω-conotoxin MVIIc ca2+ channel blocker (n, P and Q-type) 100 μg
2004 Isradipine ca2+ channel blocker (L-type) 10 mg
50 mg
2198 Mibefradil ca2+ channel blocker (T-type) 10 mg
50 mg
4507 ML 218 ca2+ channel blocker (T-type) 10 mg
50 mg
5711 nilvadipine ca2+ channel blocker (L-type); also Syk kinase inhibitor 50 mg
0600 nimodipine ca2+ channel blocker (L-type) 100 mg
2268 nnc 55-0396 highly selective ca2+ channel blocker (T-type) 10 mg
4665 ProTx I caV3.1 channel blocker; also inhibits naV1.8 and KV2.1 100 μg
2945 SnX 482 Potent and selective caV2.3 blocker (R-type) 10 μg
Others 0806 Gabapentin Selectively binds the α2δ subunit of caV channels. 10 mg
50 mg
3775 Pregabalin Selectively binds the α2δ subunit of voltage-sensitive calcium channels; anticonvulsant
10 mg
50 mg
other Calcium Channels
Activators 5586 Yoda 1 Piezo1 channel activator 10 mg
50 mg
4741 Gadolinium chloride Stretch-activated calcium channel blocker; calcium-sensing receptor agonist
50 mg
PotassiumChannelsCa2+-Activated Potassium Channels
Activators 2665 BMS 191011 Potent BKca (Kca1.1) channel opener 10 mg
50 mg
2953 cyPPa activator of Kca2.2 and Kca2.3 channels 10 mg
50 mg
1041 1-eBIo activator of epithelial Kca channels 10 mg
50 mg
4311 GW 542573X Selective activator of Kca2.1 channels 10 mg
50 mg
4788 nS 11021 activator of BKca (Kca1.1) channels 10 mg
50 mg
3804 nS 1619 activator of BKca (Kca1.1) channels 10 mg
5276 nS 19504 activator of BKca (Kca1.1) channels 10 mg
50 mg
3895 nS 309 Positive modulator of Kca2 and Kca3.1 channels 10 mg
50 mg
3670 SKa 31 activator of Kca3.1 and Kca2 channels 10 mg
50 mg
Blockers 1652 apamin Kca2 channel blocker (small conductance) 1 mg
1087 charybdotoxin Kca channel blocker (big conductance) 10 μg
1086 Iberiotoxin Kca channel blocker (big conductance) 100 μg
5571 Lei-Dab 7 high affinity, selective Kca2.2 blocker 100 μg
4864 nS 6180 Potent Kca3.1 channel blocker 10 mg
50 mg
2006 Paxilline Potent BKca channel blocker; also SeRca aTPase blocker. 10 mg
4617 Penitrem a Potent and selective BKca (Kca1.1) channel blocker 1 mg
2946 TRaM 34 Potent and highly selective Kca3.1 channel blocker 10 mg
50 mg
4952 TRaM 39 Potent Kca3.1 blocker 10 mg
50 mg
Voltage-gated Ion channels – continued
Category Cat. no. Product name Description Unit size
Tocris Product Listing Series
18 |
1310 UcL 1684 highly potent blocker of Kca2 5 mg
2661 UcL 2077 Slow afterhyperpolarization (sahP) channel blocker; sub-type selective Kv channel effects
10 mg
50 mg
Modulators 4597 nS 8593 Selective Kca2 (SK) channel negative modulator; inhibits SK currents 10 mg
50 mg
Inward Rectifier Potassium (Kir) Channels
Activators 1377 cromakalim Kir6 (KaTP) channel opener 10 mg
50 mg
0964 Diazoxide Kir6 (KaTP) channel opener; blocks desensitization of aMPa receptors 100 mg
1378 Levcromakalim Kir6 (KaTP) channel opener; active enantiomer of cromakalim (cat. no. 1377)
10 mg
50 mg
0583 Minoxidil Kir6 channel (KaTP) opener 100 mg
5380 ML 297 Selective Kir3.1/3.2 (GIRK1/2) channel activator 10 mg
50 mg
2147 nicorandil Kir6 (KaTP) channel opener and no donor 50 mg
1355 P1075 Potent Kir6 (KaTP) channel opener 10 mg
50 mg
2580 Tenidap opener of Kir2.3; also nSaID, cyclooxygenase (coX-1) inhibitor 10 mg
50 mg
2076 Y-26763 Kir6 (KaTP) channel opener 10 mg
50 mg
2077 Y-27152 Prodrug of Kir6 (KaTP) channel opener Y-26763 (cat. no. 2076); orally active in vivo
10 mg
50 mg
0882 ZM 226600 Kir6 (KaTP) channel opener 10 mg
50 mg
Blockers 3590 Gambogic acid Kir2.1 channel blocker; also activates caspases and inhibits Bcl-2 family proteins
10 mg
50 mg
0911 Glibenclamide Kir6 (KaTP) channel blocker 100 mg
2396 Glimepiride Kir6 (KaTP) channel blocker 10 mg
50 mg
4549 ML 133 Kir2 channel blocker 10 mg
50 mg
Venoms feature products
Leu-Lys-Cys-Tyr-Gln-His-Gly-Lys-Val-Val-
Thr-Cys-His-Arg-Asp-Met-Lys-Phe-Cys-Tyr-
His-Asn-Thr-Gly-Met-Pro-Phe-Arg-Asn-Leu-
Lys-Leu-Ile-Leu-Gln-Gly-Cys-Ser-Ser-Ser-
Cys-Ser-Glu-Thr-Glu-Asn-Asn-Lys-Cys-Cys-
Ser-Thr-Asp-Arg-Cys-Asn-Lys
Mambalgin 1 (5938)Selective ASIC1a inhibitor
Dendroaspis polylepsis, the Black Mamba, a source of Mambalgin 1
Venoms Venoms contain peptide toxins that are injected by an animal, via biting or stinging, into its prey. A variety of animals produce venoms, including snakes, spiders, cone snails, scorpions, bees and wasps. Many venom toxins act as blockers of ions channels and are of use in research because of their potency and high degree of selectivity for their target channel. A number of marketed medicines are based on peptides derived from animal venoms, including the analgesic ziconotide (Prialt), which originates from a cone snail and acts as a calcium channel blocker. Below is an example of an ion channel blocker, available from Tocris, which is the active ingredient of a venom.
Category Cat. no. Product name Description Unit size
By Dick culbert from Gibsons, B.c., canada – Dendroaspis polylepis – the Black Mamba, cc BY 2.0, https://commons.wikimedia.org/w/index.php?curid=50155545
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4231 nateglinide Kir6 (KaTP) blocker; displays high affinity for SUR1/Kir6.2 channels 10 mg
50 mg
2095 PnU 37883 Vascular Kir6 (KaTP) channel blocker 10 mg
50 mg
3805 Repaglinide Kir6 (KaTP) channel blocker 50 mg
0925 Sch 23390 Kir3 channel blocker; standard selective D1-like antagonist; also 5-hT2c and 5-hT1c agonist
10 mg
50 mg
4339 Tertiapin LQ Selective Kir1.1 blocker; derivative of tertiapin-Q (cat. no. 1316) 1 mg
1316 Tertiapin-Q Selective blocker of inward-rectifier K+ channels 1 mg
3891 VU 590 Inhibitor of Kir1.1 (RoMK) and Kir7.1 10 mg
50 mg
4197 VU 591 Selective Kir1.1 (RoMK) inhibitor 10 mg
50 mg
two-P Potassium Channels
Activators 3797 BL 1249 Putative K2P2.1 (TReK-1) channel opener 10 mg
50 mg
Blockers 5337 ML 365 Potent and selective TaSK-1 channel blocker 10 mg
50 mg
5338 PK-ThPP Potent TaSK-3 channel blocker 10 mg
50 mg
5594 Spadin Potent TReK-1 channel blocker 1 mg
Voltage-gated Potassium (Kv) Channels
Activators 2867 Flupirtine KV7 channel activator 10 mg
50 mg
4519 ML 213 KV7.2 and KV7.4 channel opener 10 mg
50 mg
3062 nS 1643 KV11.1 (heRG) channel activator; antiarrhythmic 10 mg
50 mg
5083 Qo 58 KV7 channel opener 10 mg
50 mg
Blockers 0940 4-aminopyridine non-selective KV channel blocker 100 mg
5659 ammTX3 KV4 channel blocker 10 μg
3489 astemizole KV11.1 (heRG) channel blocker; also orally active, potent h1 antagonist 50 mg
5929 BeKm 1 Potent and selective KV11.1 (heRG) channel blocker 100 μg
1808 e-4031 KV11.1 (heRG) channel blocker; inhibits rapid delayed rectifier K+ current (IKr)
10 mg
50 mg
5676 Guangxitoxin 1e Potent KV2.1 and KV2.2 channel blocker 100 μg
5011 hMR 1556 Potent and selective IKs channel blocker 10 mg
3899 JnJ 303 Potent and selective IKs blocker 10 mg
50 mg
3564 Kaliotoxin KV and Kca blocker 100 μg
1278 Kn 93 caM kinase II inhibitor; also K+ channel blocker (KV) 1 mg
1999 Linopirdine KV7 (KcnQ) channel blocker 10 mg
50 mg
3563 Margatoxin Potent KV1.3 channel blocker 100 μg
2000 Xe 991 Potent, selective KV7 (KcnQ) channel blocker; blocks M-currents 10 mg
50 mg
Others 2787 BaPTa aM Blocks hKV1.5, hKV11.1 (heRG) and hKV1.3 channels; also cell-permeable ca2+ chelator
25 mg
5858 Droperidol exhibits affinity for heRG channels; also D2 receptor antagonist 50 mg
non-selective / other Potassium Channels
Blockers 4739 cesium chloride Potassium channel blocker; neuroprotective 50 mg
2330 DMP 543 K+ channel blocker and potent ach release enhancer 10 mg
50 mg
Others 0416 YS-035 Inhibits K+ outward/pacemaker current 10 mg
50 mg
Voltage-gated Ion channels – continued
Category Cat. no. Product name Description Unit size
Tocris Product Listing Series
20 |
SodiumChannelsVoltage-gated sodium Channels
Activators 5941 oD1 Potent hnav1.4, rnav1.6 and rnav1.7 channel activator 10 μg
2918 Veratridine Voltage-gated na+ channel opener 10 mg
50 mg
Blockers 6159 4,9-anhydrotetrodotoxin Potent and selective nav1.6 channel blocker 100 μg
1470 Flecainide acetate cardiac na+ channel blocker; antiarrhythmic 10 mg
50 mg
4718 huwentoxin IV Selective nav1.7 channel blocker 100 μg
5066 Ica 121431 Potent and selective nav1.3 and nav1.1 channel blocker 10 mg
50 mg
5931 PF 05089771 Potent and selective nav1.7 channel blocker 10 mg
50 mg
5792 ProTx III Potent nav1.7 blocker; analgesic 100 μg
1014 QX 314 bromide na+ channel blocker 100 mg
2313 QX 314 chloride na+ channel blocker 50 mg
0768 Riluzole Blocks voltage-dependent na+ channels; also glutamate release inhibitor/GaBa uptake inhibitor
25 mg
1078 Tetrodotoxin na+ channel blocker 1 mg
1069 Tetrodotoxin citrate na+ channel blocker; citrate salt of tetrodotoxin (cat. no. 1078) 1 mg
2815 Valproic acid, sodium salt Blocks voltage-dependent na+ channels; also histone deacetylase inhibitor
100 mg
TransientReceptorPotentialChannelstRPA1
Activators 5178 aSP 7663 Selective TRPa1 activator 10 mg
50 mg
Blockers 2896 hc 030031 Selective TRPa1 blocker 10 mg
50 mg
tRPC
Activators 4522 Flufenamic acid activates TRPc6; nSaID 50 mg
Blockers 5371 clemizole TRPc5 blocker; also h1 antagonist 10 mg
50 mg
4912 GsMTx4 TRPc1 and TRPc6 blocker; inhibits mechanosensitive ion channels 100 μg
5807 M 084 TRPc4/5 channel blocker; antidepressant and anxiolytic 10 mg
50 mg
4732 ML 204 Selective TRPc4 blocker 10 mg
50 mg
3751 Pyr3 Selective TRPc3 blocker 10 mg
50 mg
tRPM
Activators 5521 cIM 0216 Selective TRPM3 agonist 10 mg
50 mg
1531 Icilin activates a novel cold receptor. cooling agent 10 mg
50 mg
3040 WS 12 TRPM8 agonist; cooling agent 10 mg
50 mg
2927 WS 3 TRPM8 agonist; cooling agent 10 mg
50 mg
Blockers 3989 aMTB TRPM8 blocker 10 mg
50 mg
5324 M8 B Potent and selective TRPM8 channel blocker 10 mg
50 mg
5143 ononetin TRPM3 blocker 50 mg
6003 PF 0515679 Selective TRPM8 blocker 10 mg
4999 9-Phenanthrol Selective TRPM4 blocker 50 mg
5388 RQ 00203078 Potent and selective TRPM8 antagonist; orally active 10 mg
50 mg
Category Cat. no. Product name Description Unit size
Ion channeLS
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5410 Tc-I 2014 Potent TRPM8 antagonist 10 mg
50 mg
4632 Tc-I 2000 TRPM8 blocker 10 mg
50 mg
tRPML
Activators 5547 MK6-83 TRPML channel activator 10 mg
50 mg
4746 ML Sa1 activator of TRPML channels 10 mg
50 mg
4907 Sn 2 Selective TRPML3 channel activator 10 mg
50 mg
tRPP
Blockers 3378 eIPa Inhibits TRPP3-mediated currents; also inhibits the na+/h+ exchanger (nhe)
10 mg
50 mg
3379 Phenamil Inhibits TRPP3-mediated currents; also inhibits epithelial na+ channels
10 mg
50 mg
tRPV
Agonists 1116 aM 404 Vanilloid receptor agonist; also anandamide transport inhibitor 10 mg
50 mg
1339 anandamide endogenous TRPV1 and cB receptor agonist 5 mg
25 mg
1017 anandamide (in Tocrisolve™ 100) endogenous TRPV1 and cB receptor agonist (in water-soluble emulsion)
10 mg
50 mg
1354 arvanil Potent TRPV1 and cB1 agonist; also anandamide transport inhibitor 5 mg
25 mg
Stem Cell feature products
NH
OMe
O
MeMe
O2N
F3C
(±)-Bay K 8644 (1544)Potent L-type (voltage-gated)
Ca2+ channel blocker
FN
O OMe
Me
O
N
HN
Mibefradil (2198)T and L-type (voltage-gated) Ca2+
channel blocker
NO2
NH
CO2Me
MeMe
MeO2C
Nifedipine (1075) L-type (voltage-gated) Ca2+
channel blocker
N O
NN
Linopirdine (1999)Voltage-gated potassium channel blocker;
blocks KV 7.1 + 7.3 (M-currents) and KV 7.1 (KCNQ1) homomeric channels
O
N N
XE 991 (2000)Potent and selective voltage-gated potassium
channel blocker. Blocks K V 7.2+7.3 (M-currents) and KV 7.1 homomeric channels
Cl
Cl
S S
NN
N
N
Yoda 1 (5586)Piezo1 channel activator
Ion Channels in Stem Cell Research:A variety of ion channels are expressed by stem cells and have recently been shown to have a role in the regulation of self-renewal, differentiation and maturation of cells. Blockade or activation of ion channels may impact on the differentiation of stem cells towards certain lineages. Pharmacological reagents targeting ion channels can also be used to characterize differentiated cells. Research in this area is of interest in tissue repair, for example wound healing or neurodegenerative diseases, disease modeling, drug target discovery and toxicity testing. Below is a selection of compounds that may be of use in determining how specific channels function to direct the differentiation of stem cells.
Voltage-gated Ion channels – continued
Category Cat. no. Product name Description Unit size
Tocris Product Listing Series
22 |
0462 (e)-capsaicin Prototypic vanilloid receptor agonist 100 mg
1556 6ʹ-Iodoresiniferatoxin high affinity TRPV1 agonist/partial agonist 1 mg
1568 naDa Vanilloid agonist; also endogenous cB1 agonist and inhibitor of Faah and aMT
5 mg
25 mg
1641 oLDa Potent, selective endogenous TRPV1 agonist 5 mg
25 mg
0934 olvanil Potent vanilloid receptor agonist 10 mg
50 mg
1466 PPahV non-pungent vanilloid receptor agonist 1 mg
1137 Resiniferatoxin Potent vanilloid receptor agonist 1 mg
3745 Rn 1747 Selective TRPV4 agonist 10 mg
50 mg
Antagonists 5781 a 425619 Potent TRPV1 antagonist 10 mg
50 mg
4319 a 784168 Potent and selective TRPV1 antagonist 10 mg
50 mg
4330 aMG 21629 Potent and selective TRPV1 antagonist 1 mg
5995 aMG 517 Potent TRPV1 antagonist 10 mg
50 mg
2316 aMG 9810 Potent and selective, competitive antagonist of TRPV1 10 mg
50 mg
2836 arachidonyl serotonin Dual TRPV1 antagonist/Faah inhibitor 10 mg
3875 BcTc TRPV1 antagonist 10 mg
50 mg
5106 GSK 2193874 Potent and selective TRPV4 antagonist; orally active 10 mg
50 mg
4100 hc 067047 Potent and selective TRPV4 antagonist 10 mg
50 mg
1975 6-Iodonordihydrocapsaicin Potent, competitive vanilloid receptor antagonist 10 mg
50 mg
3361 JnJ 17203212 Reversible, competitive and potent TRPV1 antagonist 10 mg
50 mg
1577 L-R4W2 TRPV1 antagonist peptide 1 mg
3746 Rn 1734 Selective TRPV4 antagonist 10 mg
50 mg
5678 Rn 9893 Potent and selective TRPV4 antagonist 10 mg
50 mg
1615 SB 366791 Potent, selective, competitive TRPV1 antagonist 10 mg
50 mg
3265 SB 452533 Potent TRPV1 receptor antagonist 10 mg
50 mg
4729 α-Spinasterol TRPV1 antagonist; active in vivo 1 mg
Others 5246 MRS 1477 TRPV1 positive allosteric modulator 10 mg
50 mg
2203 PaLDa endogenous lipid; potentiates effects of endovanilloids at TRPV1 receptors
10 mg
2204 STeaRDa endogenous lipid, active in vivo; enhances effects of endovanilloids at TRPV1 receptors
10 mg
1098 Tranilast Inhibits TRPV2-mediated responses; also inhibits inflammatory mediator release from mast cells
10 mg
50 mg
Category Cat. no. Product name Description Unit size
Ion channeLS
www.tocris.com | 23
The Comprehensive in Vitro Proarrhythmia Assay (CiPA) Initiative:Prior to 2005, a number of medicines were withdrawn from the market following the finding that they delayed ventricular repolarization (prolongation of the QTc interval in the ECG) causing serious arrhythmias, known as Torsades de Pointes (TdP). This life-threatening effect was found to result from the ability of these drugs to block voltage-gated potassium channels (Kv11.1 or hERG). Among drugs withdrawn from the market owing to proarrhythmic effects were: the antihistamine astemizole, the antibiotic grepafloxacin, and the treatment for gastroesophageal reflux, cisapride.
In 2005 new regulatory guidelines, E14 and ICH S7B, were introduced requiring all new drugs to be tested for their effects on the QT interval in both clinical and preclinical tests. These guidelines have proved effective in preventing the introduction of new medicines that might cause TdP. However, Kv11.1 is only one of several ion channels controlling ventricular repolarization, but E14 and ICHS7B focus only on the effect of compounds on Kv11.1 channels, so there is a possibility that these guidelines may prevent the further development of useful drugs that induce QTc prolongation, but do not increase the risk of TdP.
The Comprehensive in Vitro Proarrhythmia Assay (CiPA) initiative has been established to address this situation and aims to develop a new mechanism for assessing the proarrhythmia risk of drugs in development, with a view to revising current guidelines for approval of medicines. CiPA will have four main components: in vitro ion channel assays; computer modeling of cardiac electrophysiology; confirmation of activity in stem cell-derived cardiomyocytes; and clinical assessment of electrophysiologic effects in phase I ECG studies. For the in vitro assays, voltage clamp protocols have been developed for key cardiac ion channels, including Kv11.1, Nav1.5, Cav1.2, Kv4.3, Kir2.1, KCNQ + KCNE, to test new drugs.
In addition the CiPA steering group has generated a list of 28 drugs with known effects on cardiac electrophysiology, categorized as having high, intermediate or low risk of TdP. These drugs can be used for assay validation and calibration.
CiPA Compound Test Set
High Risk Intermediate Risk Low risk
azilimide astemizole Diltiazem
Bepridil chlorpromazine Loratadine
Dofetilide cisapride Metoprolol
Ibutilide clarithromycin Mexiletine
Quinidine clozapine nifedipine
Vandetanib Domperidone nitrendipine
Disopyramide Droperidol Ranolazine
D,L-Sotalol Terfenadine Tamoxifen
Pimozide Verapamil
Risperidone
ondansetron
QT interval
PQ S
T
R
Normal ECG Trace
Tocris Product Listing Series
24 |
AquaporinsBlockers 5412 Tc aQP1 1 aquaporin 1 (aQP1) channel blocker 10 mg
50 mg
5425 TGn 020 aquaporin 4 (aQP4) channel blocker 10 mg
50 mg
ChlorideChannelsCalcium-activated Chloride Channels
Activators 4876 eact activator of ca2+-activated cl– channel transmembrane protein 16a (TMeM16a)
10 mg
50 mg
Blockers 6076 ani 9 Potent and selective TMeM16a (anoctamin-1; ano1) blocker 10 mg
50 mg
5420 Benzbromarone TMeM16a/B calcium-activated chloride channel (cacc) blocker 50 mg
4877 caccinh-a01 calcium-activated chloride channel (cacc) inhibitor 10 mg
50 mg
5770 Monna Potent TMeM16a (anoctamin-1) blocker 10 mg
50 mg
0593 nPPB Inhibits calcium-sensitive chloride currents 50 mg
4538 T16ainh - a01 ca2+-activated cl– channel transmembrane protein 16a (TMeM16a) inhibitor
10 mg
50 mg
2510 Talniflumate cacc blocker and cl–/hco3– exchange inhibitor 10 mg
50 mg
CFtR
Activators 1422 DceBIo activates cl- conductance and hKca3.1 channels 10 mg
50 mg
Blockers 3430 cFTRinh 172 Voltage-independent, selective cFTR chloride channel blocker 10 mg
50 mg
5485 Glyh 101 Reversible, voltage-dependent cFTR chloride channel blocker 10 mg
50 mg
1646 Lonidamine cFTR cl- channel blocker; also mitochondrial hexokinase inhibitor 10 mg
50 mg
4303 PPQ 102 Potent, voltage-independent cFTR chloride channel inhibitor 10 mg
50 mg
Others 3143 KM 11060 corrects F508del-cFTR trafficking 10 mg
50 mg
3943 PG 01 cFTR mutants potentiator 10 mg
50 mg
other Chloride Channels
Blockers 1540 DcPIB Selective blocker of VSac/Icl, swell; inhibits glucose-stimulated insulin release
10 mg
50 mg
4523 DIDS cIc-Ka chloride channel blocker; TRPV1 modulator; RaD51 recombinase inhibitor
50 mg
4911 GaTx2 high affinity, selective clc-2 blocker; inhibits slow-gating 100 μg
Others 0963 9-ac chloride transport inhibitor; also inhibits PKa activated cardiac Icl 100 mg
IonophoresOthers 1234 a23187, free acid calcium ionophore 10 mg
1704 Ionomycin calcium salt calcium ionophore 1 mg
2092 Ionomycin free acid calcium ionophore 1 mg
5223 Monensin sodium salt Sodium ionophore; antibacterial agent 500 mg
4312 nigericin sodium salt Selective K+ ionophore 10 mg
2505 nonactin Monovalent cation ionophore 10 mg
3373 Valinomycin Selective K+ ionophore 10 mg
50 mg
other channelsThis group includes compounds targeting chloride channels, aquaporins (channels that allow the passage of water), ionophores (ion carrying compounds), photoswitchable ligands and compounds that modulate multiple ion channels.
Category Cat. no. Product name Description Unit size
Ion channeLS
www.tocris.com | 25
PhotoswitchableLigandsOthers 5462 aaQ chloride Photoswitchable Kv channel blocker 10 mg
50 mg
5464 ac 4 Photoswitchable TRPV1 channel blocker 10 mg
50 mg
5463 Pa 1 Photoswitchable enac blocker 10 mg
50 mg
5470 QaQ dichloride Photoswitchable nav, Kv and cav channel blocker 10 mg
50 mg
OtherChannelModulatorsOthers 4095 amiodarone Broad spectrum ion channel blocker; antiarrhythmic 50 mg
2090 caLP1 cell-permeable calmodulin agonist 1 mg
5449 erastin Mitochondria VDac modulator; also Ferroptosis activator 10 mg
3908 Ibutilide Blocks IKr, heRG and L-type ca2+ channels; class III antiarrhythmic 50 mg
1611 Lamotrigine Blocks na+, K+ and ca2+ channels; also inhibits glutamate release. anticonvulsant
10 mg
50 mg
2289 Lamotrigine isethionate Inhibits glutamate release. Water-soluble salt of lamotrigine (cat. no. 1611)
10 mg
50 mg
2314 Loe 908 Broad spectrum cation channel blocker; neuroprotective 10 mg
50 mg
2851 nefiracetam activates L/n-type calcium channels, cholinergic, monoaminergic vand GaBaergic systems; cognitive enhancer
100 mg
3692 4,4-Pentamethylenepiperidine M2 proton channel blocker 50 mg
4108 Quinidine Blocks sodium and potassium channels 50 mg
2906 TRo 19622 Binds voltage-dependent anion channel (VDac) 10 mg
50 mg
2625 Zonisamide Blocks voltage-sensitive na+ and ca2+ channels (T-type) 10 mg
50 mg
Category Cat. no. Product name Description Unit size
Scientific ReviewsProduct Guides & Listings Life Science Posters
• neurodegeneration • Pain Research• cardiovascular Research
• Learning and Memory • antidepressants • Multiple Sclerosis • Peripheral Sensitization
• nicotinic ach Receptors• neuronal 5hT Receptors• GaBa Receptors• P2X and P2Y Receptors
Other Life Science Literature from TocrisTocris also provides a wide range of scientific literature free of charge, including the following titles:
To download or request copies, please visit www.tocris.com/requestliterature
Tocris Product Listing Series
26 |
a Selection of antibodies Targeting Ion channels available from Bio-Techne
Species Molecule Description Antibody ApplicationsLigand-gated Ion Channels
epithelial sodium Channels
aF2968 Mouse Prostasin/Prss8 Mouse Prostasin/Prss8 affinity Purified Polyclonal ab eLISa capture (Matched antibody Pair), WB
aF4599 human Prostasin/Prss8 human Prostasin/Prss8 affinity Purified Polyclonal ab Ihc, IP, Simple Western, WB
MaB4599 human Prostasin/Prss8 human Prostasin/Prss8 Mab (clone 530622) Ihc, IP, WB
GABA-A Receptors
aF1188 Rat GaBa-B R2 Rat GaBa-B-R2 affinity Purified Polyclonal ab Ihc, WB
aF5590 human GaBa-a R beta 3 human GaBa-a-R beta 3 affinity Purified Polyclonal ab Ihc, Simple Western, WB
aF7000 human/Mouse/Rat GaBa-B R1 human/Mouse/Rat GaBa-B-R1 affinity Purified Polyclonal ab Ihc, WB
MaB7000 Rat GaBa-B R1 Rat GaBa-B-R1 Mab (clone 751216) Ihc
PPS022 human/Mouse/Rat/Bovine/canine/Primate/Zebrafish
GaBa-a R alpha 1 GaBa-a-R alpha 1 c-Terminus affinity Purified Polyclonal ab WB
PPS023 Mouse/Rat/Bovine GaBa-a R alpha 1 Mouse/Rat GaBa-a-R alpha 1 n-Terminus affinity Purified Pab WB
PPS024 human/Mouse/Rat/Bovine/canine/Primate
GaBa-a R alpha 2 human/Mouse/Rat/Bovine GaBa-a-R alpha 2 Polyclonal ab WB
PPS025 human/Mouse/Rat/Bovine/canine/Primate/Zebrafish
GaBa-a R alpha 4 GaBa-a-R alpha 4 c-Terminus affinity Purified Polyclonal ab WB
PPS027 Mouse/Rat GaBa-a R alpha 5 Mouse/Rat GaBa-a-R alpha 5 c-Terminus affinity Purified Pab WB
PPS030 human/Mouse/Rat GaBa-a R beta 1 GaBa-a-R beta 1 c-Terminus affinity Purified Polyclonal ab WB
PPS031 human/Mouse/Rat/Bovine/canine/Primate
GaBa-a R beta 2 GaBa-a-R beta 2 c-Terminus affinity Purified Polyclonal ab WB
PPS072 human/Mouse/Rat/Bovine/chicken/Primate/Zebrafish
GaBa-a R gamma 2 human/Mouse/Rat/Bovine GaBa-a-R gamma 2 Polyclonal ab WB
PPS073 human/Mouse/Rat/Xenopus GaBa-B R2 Phospho-GaBa-B-R2 (S892) affinity Purified Polyclonal ab IF, WB
PPS090 human/Mouse/Rat/Bovine GaBa-a R delta GaBa-a-R delta n-Terminus affinity Purified Pab Ihc, IP, WB
Ionotropic Glutamate Receptors
aF4514 human mGluR5 human mGluR5 affinity Purified Polyclonal ab Ihc, WB
aF4668 human mGluR3 human mGluR3 affinity Purified Polyclonal ab Ihc, WB
aF4836 human mGluR1 human mGluR1 affinity Purified Polyclonal ab WB
aF7387 human mGluR4 human mGluR4 affinity Purified Pab cyToF-ready, Flow cytometry, Ihc
aF8138 human hcn4 human hcn4 affinity Purified Polyclonal ab Icc
MaB4405 human mGluR7 human mGluR7 Mab (clone 437310) cyToF-ready, Flow cytometry
MaB4514 human mGluR5 human mGluR5 Mab (clone 464818) cyToF-ready, Intracellular Staining by Flow cytometry, WB
MaB45141 human mGluR5 human mGluR5 Mab (clone 464823) Ihc
MaB4676 human mGluR2 human mGluR2 Mab (clone 455310) cyToF-ready, Intracellular Staining by Flow cytometry, WB
MaB4836 human mGluR1 human mGluR1 Mab (clone 511622) Ihc
MaB5277 human mGluR8 human mGluR8 Mab (clone 476410) Ihc, WB
MaB8138 human hcn4 human hcn4 Mab (clone 880904) Icc
PPS007 human/Mouse/Rat/canine/chicken
GluR1 Phospho-GluR1 (S831) affinity Purified Polyclonal ab WB
PPS008 human/Mouse/Rat/Primate GluR1 Phospho-GluR1 (S845) affinity Purified Polyclonal ab WB
PPS009 Rat Glycine R Rat Glycine R affinity Purified Polyclonal ab Ihc, WB
PPS011B human/Mouse/Rat GRIn1/nMDaR1 human/Mouse/Rat GRIn1/nMDaR1 Mab (clone R1JhL) IP, WB
PPS033 human/Mouse/Rat GRIn2c/nMDaR2c human/Mouse/Rat GRIn2c/nMDaR2c affinity Purified Pab IP, WB
PPS051 human/Mouse/Rat/chicken/Zebrafish
GluR2/3 human/Mouse/Rat GluR2/3 affinity Purified Polyclonal ab WB
PPS080 Mouse/Rat GRIn1/nMDaR1 Mouse/Rat GRIn1/nMDaR1 Variant c1 affinity Purified Pab Ihc, WB
PPS081 Mouse/Rat GRIn1/nMDaR1 Mouse/Rat GRIn1/nMDaR1 Variant c2 affinity Purified Pab Ihc, WB
PPS082 human/Mouse/Rat GRIn1/nMDaR1 GRIn1/nMDaR1 Variant c2’ affinity Purified Polyclonal ab Ihc, WB
PPS083 Mouse/Rat GRIn1/nMDaR1 Mouse/Rat GRIn1/nMDaR1 Variant n1 affinity Purified Pab Ihc, WB
Voltage-gated Ion Channels
Potassium Channels
aF2360 human DPP6 human DPP6 affinity Purified Polyclonal ab cyToF-ready, Flow cytometry, Ihc, IP, WB
MaB2360 human DPP6 human DPP6 Mab (clone 274308) cyToF-ready, Flow cytometry, IP
MaB23601 human DPP6 human DPP6 ectodomain Mab (clone 274311) IP, WB
MaB4100 human DPP10 human DPP10 Mab (clone 453601) WB
PPS015 Rat/Xenopus Potassium channel Kv2.2
Potassium channel Kv2.2 affinity Purified Pab Ihc, WB
PPS016 Mouse/Rat Potassium channel Kv3.1
Phospho-Potassium channel Kv3.1 (S503) affinity Purified Pab Ihc, WB
other Channels
CFtR
MaB1660 human cFTR human cFTR R Domain Mab (clone 13-1) IF, Ihc, IP, WB
MaB25031 human cFTR human cFTR c-Terminus Mab (clone 24-1) Ihc, IP, WB
Icc, immunocytochemistry; IF, immunofluorescence; Ihc, immunohistochemistry; IP, immunoprecipitation; WB, Western Blot.
Find out more at bio-techne.com
Ion channeLS
www.tocris.com | 27
References
Category Authors Year Title Journal Vol Page
Pharmacology clapham et al. 2003 International Union of Pharmacology. XLIII. compendium of voltage-gated ion channels: transient receptor potential channels.
Pharmacol.Rev. 55 591
Goldstein et al. 2005 International Union of Pharmacology. LV. nomenclature and molecular relationships of two-P potassium channels.
Pharmacol.Rev. 57 527
Gutman et al. 2005 International Union of Pharmacology. LIII. nomenclature and molecular relationships of voltage-gated potassium channels.
Pharmacol.Rev. 57 473
Verkman and Galietta
2009 chloride channels as drug targets. Nat.Rev.Drug.Discov. 8 153
Kellenberger and Schild
2014 International Union of Basic and clinical Pharmacology Review. XcI. Structure, function, and pharmacology of acid-sensing channels (aSIcs) and the epithelial na+ channel.
67 1
Boscardin et al. 2016 International Union of Basic and clinical Pharmacology Review. The function and regulation of acid-sensing channels (aSIcs) and the epithelial na+ channel (enac): IUPhaR review 19.
Br.J.Pharmacol. 173 2671
Ion Channels in Cancer Research
Djamgoz et al. 2014 Theme Issue. Ion transport and cancer: from initiation to metastasis.
Philos.Trans.R.Soc.B. Biol.Sci.
369
Ion Channels in Immunology Research
Feske et al. 2012 Ion channels and transporters in lymphocyte function and immunity.
Nat.Rev.Immunol. 12 532
Feske et al. 2015 Ion channels in innate and adaptive immunity. Annu.Rev.Immunol. 33 291
Vig and Kinet 2009 calcium signaling in immune cells. Nat.Immunol. 10 21
Stebbing et al. 2015 The role of ion channels in microglial activation and proliferation – a complex interplay between ligand-gated ion channels, K+ channels, and intracellular ca2+.
Front.Immunol. 6 497
Ion Channels in Stem Cell Research
Pathak et al. 2014 Stretch-activated ion channel Piezo1 directs lineage choice in human neural stem cells.
Proc.Natl.Acad.Sci.U.S.A. 111 16148
nguemo et al. 2013 The L-type ca2+ channel blocker nifedipine represses mesodermal fate determination in murine embryonic stem cells.
PLoS One 8 e53407
Iannotti et al. 2009 expression, localization, and pharmacological role of KV7 potassium channels in skeletal muscle proliferation, differentiation, and survival after myotoxic insults.
J.Pharmacol.Exp.Ther. 332 811
Zhou et al. 2011 Potential role of KcnQ/M-channels in regulating neuronal differentiation in mouse hippocampal and embryonic stem cell-derived neuronal cultures.
Exp.Neurol. 229 471
Rodríguez-Gómez et al.
2012 T-type ca2+ channels in mouse embryonic stem cells: modulation during cell cycle and contribution to self-renewal.
Am.J.Physiol.Cell Physiol. 302 c494
Ge et al. 2013 Distal c terminus of caV1.2 channels plays a crucial role in the neural differentiation of dental pulp stem cells.
PLoS One 8 e81332
CiPA colatsky et al. 2016 The comprehensive in vitro proarrhythmia assay (ciPa) initiative – update on progress.
J.Pharmacol.Toxicol.Methods
81 233
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