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 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.

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

(5R)-BW-4030W92, the active enantiomer of BW-4030W92, is an orally available, non-selective, voltage-dependent, and use-dependent sodium channel antagonist used in the study of neurological disorders.

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.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.

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.

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).

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

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.

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.

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.

JNJ-26489112 is a CNS-active agent and inhibitor of voltage-gated Na+ channels and N-type Ca2+ channels with broad-spectrum anticonvulsant activity in rodents and can be used to study neurological disorders.

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.

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.

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

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

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.

Ropivacaine hydrochloride (Ropivacaine monohydrochloride) is the hydrochloride salt of ropivacaine, a local anesthetic of the amide type with analgesic activity.

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.

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.

VX-150 is a highly selective NaV1.8 inhibitor relative to the other sodium channel subtypes (>400-fold).

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.

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