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.

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1/26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

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.

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

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].

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.

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

Guanosine 5'-diphosphate (GDP) as Potential Iron Mobilizer, Preventing the Hepcidin-Ferroportin Interaction and Modulating the Interleukin-6/Stat-3 Pathway.

Hymenidin, an alkaloid isolated from the Okinawan sponge Hymeniacidon sp. is a 5-hydroxytryptaminergic receptor antagonist and voltage-gated potassium channel inhibitor with potential antiprotozoal effects.It selectively binds to FOXO1 DNA and reduces depolarization-induced elevation of cellular calcium.

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.

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.

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).

Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochloride can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long-term treatment.

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).

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.

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.

Ursodeoxycholic acid (UDCA) is a potent inhibitor of liver-specific fatty acid transporter 5 (FATP5). Ursodeoxycholic acid inhibits cholesterol absorption and is used to dissolve gallstones.

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.

Sulfatinib (KDR-IN-1) (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC 50 s ranging from 1 to 24 nM.

CM-TPMF is a highly efficient and potent activator of the K(Ca)2.1 channel, with an EC50 value of 24 nM for (-)CM-TPMF, which exerts its activating effect through Ser293 in the transmembrane segment 5, and can be used for research into related neurological disorders.

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

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

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.

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