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Ion Channels

Ion Channels

XE 991 dihydrochloride

XE 991 dihydrochloride is a potent and selective blocker of KV7 (KCNQ) voltage-gated potassium channels. Blocks KV7.2+7.3 (KCNQ2+3) / M-currents (IC50 = 0.6 - 0.98 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 0.75 μM) but is less potent against KV7.1/minK channels (IC50 = 11.1 μM). Learn More

Starting at: $110.00

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SR 33805 oxalate

SR 33805 oxalate is a potent Ca2+ channel antagonist which binds allosterically to the a1-subunit of L-type Ca2+ channels (Kd = 20 pM), at a site distinct from other types of blocker. It also inhibits PDGF-stimulated smooth muscle cell proliferation. Learn More

Starting at: $150.00

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TC-N 1752

TC-N 1752 is a selective blocker of human NaV1.7 channels (IC50 values are 0.17, 0.3, 0.4 and 1.1 μM at hNaV1.7, hNaV1.3, hNaV1.4 and hNaV1.5 respectively), which also displays analgesic efficacy in the formalin pain model and inhibits tetrodotoxin-sensitive sodium channels. Learn More

Starting at: $155.00

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FPL 64176

FPL 64176 is a potent activator of L-type Ca2+ channels (EC50 = 16 nM). Learn More

Starting at: $85.00

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Amlodipine besylate

Amlodipine besylate is a L-type calcium channel blocker that displays antihypertensive properties, which inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease. Learn More

Starting at: $50.00

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Ruthenium Red

Ruthenium Red Blocks Ca2+ uptake and release from mitochondria, and Ca2+ release from ryanodine-sensitive intracellular stores. Also blocks cell membrane-located capsaicin-activated cation channels (IC50 = 14 nM) and voltage-sensitive Ca2+ channels to inhibit neurotransmitter release. Learn More

Starting at: $65.00

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Efonidipine hydrochloride monoethanolate

Efonidipine hydrochloride monoethanolate is a selective blocker of L-type and T-type Ca2+ channels which displays minimal inhibition of N- and P/Q-type channels and no inhibition of R-type channels. Learn More

Starting at: $85.00

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OLDA

OLDA is a potent endogenous vanilloid TRPV1 (VR1) receptor agonist (EC50 = 36 nM at hVR1) with low affinity for rCB1 receptors (Ki = 1.6 μM). Learn More

Starting at: $75.00

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Linopirdine dihydrochloride

Linopirdine dihydrochloride is a blocker of KV7 (KCNQ) voltage-gated potassium channels; blocks KV7.1+7.3 (KCNQ2+3) / M-currents (IC50 = 4 - 7 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 8.9 μM). Learn More

Starting at: $115.00

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L-364,373

L-364,373 is a activator of KV7.1 (KCNQ1) channels. Learn More

Starting at: $140.00

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RN 1747

RN 1747 is a selective TRPV4 agonist (EC50 values are 0.77, 4.0 and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively) which displays selectivity over other TRP channels (EC50 values are 0.77, >30, >30 and >100 μM for TRPV4, TRPM8, TRPV3 and TRPV1 receptors respectively). Learn More

Starting at: $95.00

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PALDA

PALDA is an endogenous fatty acid dopamide that displays 'entourage' effects on endovanilloids NADA and anandamide. Learn More

Starting at: $75.00

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UK 78282 hydrochloride

UK 78282 hydrochloride is a blocker of the KV1.3 and KV1.4 voltage-gated potassium channels in T lymphocytes (IC50 values are 0.28 and 0.17 μM respectively). Learn More

Starting at: $135.00

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PPAHV

PPAHV is a non-pungent vanilloid TRPV1 (VR1) receptor agonist (Ki = 3.1 μM) that displays non-cooperative binding and induces apoptosis via a non-VR1 mechanism in Jurkat cells and causes vasoconstriction in vivo. Learn More

Starting at: $98.00

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NS 3623

NS 3623 is a human ether-a-go-go (hERG) KV11.1 potassium channel activator, which activates the IKr current and displays antiarrhythmic activity and exhibits potential dual mode of action at the hERG inhibitory site; may also act as a partial blocker of KV11.1 (hERG) channels. Learn More

Starting at: $145.00

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6'-Iodoresiniferatoxin

6'-Iodoresiniferatoxin is a high affinity TRPV1 (VR1) vanilloid receptor partial agonist (Ki = 0.71 nM; EC50 = 130 nM at human VR1), which displays partial agonism at human VR1 and full agonism at rat VR1. Learn More

Starting at: $159.00

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ICA 110381

ICA 110381 is a KV7.2/7.3 activator (EC50 = 0.38 μM), which decreases neuronal excitability in CA1 hippocampal neurons. Exhibits anticonvulsive properties in amygdala-kindled rats, a model for complex partial seizures. Learn More

Starting at: $99.00

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PD 118057

PD 118057 is a human ether-a-go-go (hERG) KV11.1 potassium channel activator, which displays no major effect on INa, ICa/L, IK1 and IKs currents. Learn More

Starting at: $119.00

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Licarbazepine

Licarbazepine is an active metabolite of oxcarbazepine which produces dose-dependent inhibition of glutamatergic excitatory postsynaptic potentials (EPSPs). Learn More

Starting at: $85.00

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Ambroxol hydrochloride

Ambroxol hydrochloride is a sodium channel blocker and mucolytic agent with antioxidant, anti-viral and anti-inflammatory properties, which inhibits tetrodotoxin (TTX)-resistant channels more potently than TTX-sensitive subtypes (IC50 values for tonic block are 35.2 and 111.5 μM respectively). Learn More

Starting at: $69.00

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