Sodium Channel

Suzetrigine（VX-548） is an orally active and specific NaV1.8 inhibitor. Suzetrigine has analgesic activity and can be used to study acute pain and neurotransmission.

Sulcardine sulfate (B-87823) is a multi-ion channel blocker with antiarrhythmic activity, inhibits Na+, K+ and Ca2+ channels, and inhibits hNav1.5 channels in a concentration-dependent and reversible manner.

Sulcardine 2HCl is a multi-ion channel blocker with antiarrhythmic effects that blocks the properties of hERG and hNav1.5 channels and can be used to study atrial fibrillation and ventricular arrhythmias.

Homoeriodictyol, a naturally occurring, bitter-masking flavanone, as a promising agent to increase appetite and food intake. The flavanone homoeriodictyol can increase SGLT-1-mediated glucose uptake but decrease serotonin release in differentiated Caco-2 cells.

SM-6586 is a potent calcium channel antagonist with inhibitory effects on Na+ H+ and Na+ Ca2+ exchange channels, and can be used in the study of cerebrovascular disease and hypertension, among other diseases.

Tenapanor (RDX 5791) is an inhibitor of the sodium-proton (Na(+)/H(+)) exchanger NHE3, which plays a prominent role in sodium handling in the gastrointestinal tract and kidney. Tenapanor possesses an excellent preclinical safety profile and, as of now, there are no serious concerns about its side effects.

AZD 7009 is a novel antiarrhythmic compound that inhibits the sodium current of hNav1.5 in CHO K1 cells with an IC50 of 11 uM. AZD 7009 inhibited late sodium current in isolated rabbit atrial and ventricular myocytes, and prolonged E-4031-induced action potential duration, promoting early post-depolarization of Purkinye fibers (EADs).

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

PF-06305591 is an effective and selective blocker of voltage-gated sodium channel NaV1.8 (IC50 = 15 nM).

R 56865 is a weak potential-operated channel inhibitor that inhibits the late sodium current in human isolated cardiomyocytes.

E 0747 (E0747) is a new antiarrhythmic compound that inhibits arrhythmias by inhibiting Na channels in cardiac cells.

GX 201 is a selective NaV1.7 inhibitor, IC50 of < 3.2 nM for hNaV1.7.

KT-362 fumarate is a novel compound that acts as an antagonist of calcium channels, potassium channels and sodium channels.KT-362 fumarate causes vasodilation by affecting intracellular calcium mobilization in atrial muscle cells.KT-362 fumarate has a relaxing effect on femoral and basilar artery strips in rabbits.

GNE-131 is a potent and specific inhibitor of human sodium channel NaV1.7 (IC50: 3 nM).

Camostat mesylate (FOY-S980) is a trypsin-like protease inhibitor and inhibits airway epithelial sodium channel (ENaC) function.

20(S)-Ginsenoside Rg3 (Rg3) possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells. It inhibits the proliferation of human umbilical vein endothelial cells(HUVEC) and has anti-angiogenesis activities.

Sipatrigine (619C89) is an antiepileptic compound with neuroprotective activity through glutamate release, TREK ion channels, TRESK channels, sodium channels, and calcium channel inhibitors in the CNS, and can be used to study TRESK channels.

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, with little or no activity against human Nav1.5 or Nav1.7 channels.

GX-585 is a sulfonamide analog that is a Nav 1.7 channel inhibitor with analgesic activity for the study of neuropathic pain and inflammation.

1. Oleandrin (Folinerin), the principal cardiac glycoside component of PBI-524, can quantitatively account for regulation of BDNF at both the protein and transcriptional levels. 2. Oleandrin are known to inhibit the Na, K-ATPase pump, resulting in a consequent increase in calcium influx in heart muscle. 3. Oleandrin has stronger anti-proliferative activity in undifferentiated CaCO-2 cells (IC50, 8.25 nM) , causes an autophagic cell death and altered ERK phosphorylation in undifferentiated.

Pilsicainide HCl (SUN 1165) is a pure sodium channel blocker

Funapide (TV 45070) is a potent Sodium Channel Nav1.7 inhibitor with potential anti-inflammatory activity for the treatment of erythema gangrenosum, musculoskeletal pain, knee osteoarthritis, and postherpetic nerves.

Rimeporide hydrochloride (EMD-87580 hydrochloride) is a potent and selective inhibitor of Sodium hydrogen exchange 1 (NHE-1).

EIPA (L593754) is a TRPP3 channel inhibitor (IC50=10.5 μM) and an inhibitor of Na+ H+ exchange (NHE). EIPA inhibits megacytosis, promotes autophagy, and can be used in inflammation and tumor studies.

Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.

Halofuginone (RU-19110), the competitive inhibitor of prolyl-tRNA synthetase(Ki=18.3 nM), could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng ml in the mammal.

BIIB 722 Mesylate is a selective sodium-hydrogen exchange inhibitor with cardioprotective properties and can be used to study myocardial ischemia and myocardial infarction.

Elpetrigine (GW273293) is a potential sodium channel blocker with antiepileptic activity that can be used to study epilepsy.

SB-237376 HCl (SB-237376 hydrochloride) is a calcium and potassium channel antagonist used in the treatment of cardiac arrhythmias.

Besipirdine (HP 749 free base) is a non-receptor-dependent cholinomimetic compound with alpha-adrenergic and cardiovascular activities.Besipirdine inhibits voltage-dependent sodium-potassium channels and inhibits biogenic amine uptake.Besipirdine reduces schedule-induced irritability and thirst and enhances cholinergic and adrenergic activity in the CNS in the rat. Besipirdine reduces schedule-induced thirst and enhances cholinergic and adrenergic neurotransmission in the central nervous system.

Riluzole (RP-54274) is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.

(+)-Kavain ((R)-KAWAIN) is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B.

PF-06869206 is an oral selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1, IC50: 380 nM).

Dimethyl lithospermate B (dmLSB) is a selective Na+ channel agonist.

QX-314 chloride is a membrane-impermeable, permanently charged blocker of the sodium channel.

Veratridine is a benzoate-cevane found in Veratrum and Schoenocaulon. It activates sodium channels to stay open longer than normal.

PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.

Ralitoline (Ralitolinum) is an anticonvulsant with anticancer activity and sodium channel blocking activity.

(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379, an orally active and selective sulfonamide NaV1.7 antagonist.

PF-05186462 (PF-05150122) is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.

LTGO-33 is a species-specific inhibitor of the voltage-gated sodium channel NaV1.8, inhibiting NaV1.8, NaV1.1-NaV1.7, and NaV1.9.LTGO-33 inhibits wild-type and multiple NaV1.8 variants associated with human pain disorders and can be used for the study of pain.hBChE-IN-2 is a low affinity Nurr1 agonist.

Nefopam hydrochloride (Nefopam HCl) is the hydrochloride salt form of nefopam, a centrally-acting, non-opioid benzoxazocine with analgesic activity.

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Zandatrigine (NBI-921352) is a sodium channel protein type 8 subunit alpha blocker, suitable for studies on epilepsy treatment and nervous system pathologies.

DS-1971a is a highly potent and selective NaV1.7 inhibitor. DS-1971a exhibits a favorable toxicological profile and analgesic effects.

Crobenetine (BIII 890 CL) Free Base is a selective NaV channel blocker that eliminates VTD-induced [Ca2+] elevation.

Propafenone (Propafenonum) is only found in individuals that have used or taken this drug. It is an antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated. The electrophysiological effect of propafenone manifests itself in a reduction of upstroke velocity (Phase 0) of the monophasic action potential. In Purkinje fibers, and to a lesser extent myocardial fibers, propafenone reduces the fast inward current carried by sodium ions, which is responsible for the drugs antiarrhythmic actions. Diastolic excitability threshold is increased and effective refractory period prolonged. Propafenone reduces spontaneous automaticity and depresses triggered activity. At very high concentrations in vitro, propafenone can inhibit the slow inward current carried by calcium but this calcium antagonist effect probably does not contribute to antiarrhythmic efficacy.

Carbamazepine (NSC-169864) is a tricyclic compound chemically related to tricyclic antidepressants (TCA) with anticonvulsant and analgesic properties. Carbamazepine exerts its anticonvulsant activity by reducing polysynaptic responses and blocking post-tetanic potentiation. Its analgesic activity is not understood; however, carbamazepine is commonly used to treat pain associated with trigeminal neuralgia.