potassiumchannel

Gut restricted-7 (GR-7) is a potent, covalent, orally administered, gut-selective bile salt hydrolase (BSH) inhibitor with tissue specificity that localizes to the gut. Gut restricted-7 reduces BSH activity in gut bacteria and decreases levels of unconjugated bile acids in mouse feces, making it suitable for research into metabolism, inflammation, and intestinal diseases.

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

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.

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

Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase through K+-competitive binding, with an IC50 of 1.0 μM.

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).

Kv3 modulator 1 is an imidazolidinedione-type orthosteric modulator of Kv3 voltage-gated potassium channels. Kv3 modulator 1 reverses mechanical hyperalgesia in rat models of neuropathic and inflammatory pain, with rapid onset and sustained, dose-dependent effects. Kv3 modulator 1 can be used to study the mechanisms underlying inflammatory pain and neurological disorders such as epilepsy and schizophrenia.

OR-1896 is the active metabolite of Levosimendan, a highly specific phosphodiesterase (PDE III) inhibitor, a vasodilator with partial anti-inflammatory properties that produces vasodilation in different types of blood vessels through activation of ATP-sensitive (KATP) and other potassium channels.OR-1896 can be used to study heart failure and vascular dysfunction. OR-1896 can be used to study heart failure and vascular dysfunction.

(+)-KCC2 blocker 1 is a selective inhibitor of KCC2 with an IC50 of 0.4 μM.

PD-118057 is a potent ether associated (hERG) potassium channel activator that shows no activity against hERG. PD-118057 inhibits the excitability of the membrane by activating the hERG channel. PD-118057 is a potential compound for the treatment of delayed repolarization in inherited or acquired long QT syndrome and congestive heart failure.

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.

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.

AVE-0118 is a potassium channel blocker and suppresses persistent atrial fibrillation.

Bisaramil hydrochloride (Bisaramil) is a novel diazabicyclononane antiarrhythmic compound that inhibits the generation of free radicals.Bisaramil hydrochloride blocks sodium currents and inhibits the slow Ca(2+) action potential induced by isoproterenol in K(+)-depolarized muscle.

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.

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

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

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

Dimethindene (Dimetindeno) is a selective antagonist of H1 receptor and blocks K+ current. Dimethindene exhibits antihistamine and anticholinergic effects.

Vesnarinone HCl (OPC-8212 HCl) is an orally active phosphodiesterase 3 (PDE3) inhibitor.Vesnarinone HCl modulates calcium and potassium ions, increasing calcium flux and decreasing potassium flux.Vesnarinone HCl is a new positive inotropic compound that enhances myocardial contractility and can be be used in heart failure studies.

GAL-021 an intravenous BKCa-channel blocker.

GAL-021 sulfate is a BKCa channel blocker that inhibits the analgesic effects of opioids and is used in the study of respiratory control diseases.

ML353 (VU0478006) is a selective activator of TREK-1 and TREK-2 and a selective ligand (Ki =18.2 nM) for the mGlu5 Silencing Allosteric Modulator (SAM). ML353 has potential as a solution to the intrinsic activity or pharmacological blockade of SAM in vivo.

Celivarone is a potassium channel blocker used in the study of arrhythmias, atrial flutter and atrial fibrillation.