Potassium Channel

Nigericin sodium salt is an antibiotic, an NLRP3 activator, and a cationic ion carrier. Nigericin sodium triggers the activation of the NALP3 inflammasome, which inhibits Golgi function and suppresses the growth of Gram-positive bacteria.

Kv3 modulator 1 is a voltage-gated potassium channel Kv3 modulator that can be used to study neurologic-level diseases.

Branaplam (LMI 070) is a highly potent, selective and orally active small molecule SMN2 splicing modulator.

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.

Gut restricted-7 (GR-7) is a covalent and orally active pan-bile salt hydrolase (BSH) inhibitor that reduces gut bacterial BSHs and decreases deconjugated bile acid levels in the feces of mice.

BAPTA-AM is a calcium chelator that is cell-permeable and selective, blocking hERG, hKv1.3, and hKv1.5 channels (IC50=1.3 1.45 1.23 μM). BAPTA-AM has a 105-fold higher affinity for Ca2+ than for Mg2+, and can be used for the role of calcium in cell signaling.

Atpenin A5 is a potent and highly specific complex II inhibitor (IC50 ~10 nM), as well as an effective mKATP channel agonist and cardioprotective agent [1].

SCH-23390 hydrochloride (R-(+)-SCH23390 hydrochloride) is an effective dopamine receptor antagonist, with high affinity for the D1 (Ki=0.2 nM) and D5 (Ki=0.3 nM) receptors.

BMS-919373 is a potassium channel Kv1.5 (KCNA5) inhibitor for atrial fibrillation and acute coronary syndrome.

BSH-IN-1 is a potent, covalent inhibitor of gut bacterial recombinant bile salt hydrolases (BSHs; IC50s: 108 nM for B. longum BSH and 427 nM for B. theta BSH).

Rosuvastatin (ZD4522) is an inhibitor of HMG-CoA reductase (HMGCR) (IC50=11 nM), selective and competitive. Rosuvastatin has hypolipidemic and antiatherosclerotic effects.

PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a selective, orally active Kv1.3 blocker with an EC50 of 2 nM.

E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM)

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.

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.

DCPIB, a known specific and potent inhibitor of volume-regulated anion channels (VRAC),DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1 TRAAK channels.

Tetrandrine (Sinomenine A) is a naturally occurring biphenylisoquinoline alkaloid, a calcium channel inhibitor. Tetrandrine inhibits voltage-gated calcium channels (ICa) and Ca2+-activated potassium channels.

Ursodeoxycholic acid (UDCA) can be used to dissolve gallstones and reduce cholesterol absorption.

Minoxidil sulfate (U-58838) is the active metabolite required to exert the vasodilatory and hair growing effects of minoxidil.

KCNQ2 3 activator-1 is a Kv7.2 Kv7.3 (KCNQ2 3) potassium channel activator, details of which are from Compound A of Patent WO2021113757A1.

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.

Levosimendan (OR1259) is a calcium sensitizer used in the management of acutely decompensated congestive heart failure. It increases the sensitivity of the heart to calcium, thus increasing cardiac contractility without a rise in intracellular calcium. Levosimendan exerts its effect by increasing calcium sensitivity of myocytes by binding to cardiac troponin C in a calcium-dependent manner.

Daurisoline ((R,R)-Daurisoline) is a hERG inhibitor. Daurisoline is also an autophagy blocker.

MK-0448 is a novel and selective blocker of the Kv1.5 (KCNA5) channel, a key channel involved in cardiac repolarization that is associated with atrial-specific ultra-rapid K+ current I Kur.

Aprikalim (RP 52891) is an adenosine triphosphate potassium channel (KATP) opener that protects against nerve damage in a rabbit model of spinal cord ischemia.Aprikalim inhibits vasoconstriction and inhibits the elevation of [Ca2+]i during myocardial paralysis, and can be used to study cardiovascular disease.

Tertiapin-Q is a bee toxin derivative that inhibits BK-type K(+) channels in a concentration-dependent manner and inhibits efflux to K(+).

Tannic acid (Gallotannic acid) is a novel hERG channel blocker.

Tolazamide (U-17835) is a sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.

ZTZ240 is a KCNQ2 channel activator used in the study of epilepsy.

UK 66914 is a K(+) channel blocker for the study of cardiac arrhythmias.

Pimozide (R6238) is a diphenylbutylpiperidine derivative and a dopamine antagonist with the antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), thereby decreasing dopamine neurotransmission and reducing the occurrence of the motor and vocal tics and delusions of parasitosis. In addition, this agent antagonizes alpha-adrenergic and 5-HT2 receptors.

Strictosamide possesses antibacterial and antiviral activities, it also may have important effects on inflammation and inflammatory pain.

C 101248 (KCNK13-IN-1) is a selective and potent tandem pore halogen inhibitor of K+ channel 1 (THIK-1) inhibitor and human and mouse KCNK13 inhibitor.C 101248 inhibits IL-1β release in a concentration-dependent manner and can be used for the study of inflammation induced by neurodegenerative disorders.

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.

Dofetilide (UK 68789) is a sulfonamide class III antiarrhythmic agent and potassium channel blocker. Dofetilide selectively blocks cardiac ion channels of the rapid component of the delayed rectifier potassium current Ikr. This antiarrhythmic agent prolongs cardiac action potential duration and effective refractory period due to delayed repolarization without affecting conduction velocity. This results in a normal sinus rhythm. Dofetilide is used in the treatment of atrial fibrillation and flutter.

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

IK1 inhibitor PA-6 (PA-6) is a selective and potent inhibitor of IK1 (KIR2.x ion-channel-carried inward rectifier current) with an IC50 of 12-15 nM for human and mouse KIR2.x currents.

Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.

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

Maralixibat Chloride (LUM001 chloride), an apical, sodium-dependent, bile acid transport inhibitor, prevents enterohepatic bile acid recirculation.

Nifedipine (Procardia) is a dihydropyridine calcium channel blocking agent. Nifedipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in some multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents.

Novobiocin Sodium (Albamycinsodium) binds to DNA gyrase and blocks adenosine triphosphatase (ATPase) activity. Novobiocin sodium is an antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin.

Chenodeoxycholic acid (CDCA) is a bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.

Rosuvastatin calcium (ZD4522) , a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity.

Linoleoyl glycine, a modified polyunsaturated fatty acid, is an endogenous homologue of linoleoyl glycine. Linoleoyl glycine activates human KCNQ1 KCNE1 (hKCNQ1 hKCNE1) channels expressed in xenopus oocytes from mammalian skin, spinal cord and brain, and has shown analgesic activity in animal studies.

CLP290 is an activator of the neuron-specific K+-Cl cotransporter KCC2 and displays potential for the treatment of a wide range of neurological and psychiatric indications.

NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.

ASP-2905 is a potent and selective inhibitor of potassium channel Kv12.2 encoded by the Kcnh3 BEC1 gene. It can cross the blood-brain barrier and has antipsychotic activities