herg potassium channel

A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator that enhances hERG currents by slowing inactivation, promoting activation, reducing inactivation, and shortening atrial and ventricular repolarization in a complex manner.

Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression.

Cavutilide has antiarrhythmic activity, inhibits hERG K(+) channels, and can be used to study heart failure and persistent atrial fibrillation.

Naluzotan hydrochloride (PRX 00023 hydrochloride) is a hERG K+ channel blocker with an IC50 value of 3800 nM and is commonly used in the study of anxiety and depression.Naluzotan hydrochloride is also a novel, potent, and selective 5-HT1A agonist, with an IC50 value of about 20 nM and a Ki value of about 5.1 Naluzotan hydrochloride is also a novel, potent and selective 5-HT1A agonist with an IC50 of approximately 20 nM and a Ki of approximately 5.1 nM.

Cloperastine fendizoate (Hustazol) inhibits the hERG K+ currents in a concentration-dependent manner (IC50: 27 nM).

Endoxifen Z-isomer (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.

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

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

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.

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

Cisapride (R 51619) is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal peristalsis, increase gastric emptying and decrease esophageal reflux.

MCHR1 antagonist 2 is an inhibitor of melanin-concentrating hormone receptor 1 (MCH1-R, IC50 = 65 nM) and also inhibits hERG.

Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current.

Terfenadine ((±)-Terfenadine) is a prodrug metabolized by intestinal CYP3A4 into fexofenadine, an active selective histamine H1-receptor antagonist that possesses antihistaminic and non-sedative effects.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

Halofantrine hydrochloride (SKF-102886) is an orally administered antimalarial drug effective against drug-resistant P. falciparum and P. vivax. SKF-102886 has cardiac toxicity, inhibiting hERG and delayed rectifier potassium channel I Kr, leading to prolonged QTc and PR intervals.

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

GLP-1 receptor agonist 15 (Example 4) is a GLP receptor agonist with an EC50 of 0.74 nM. It exhibits an IC50 of 10.1 μM against the hERG potassium ion channel. This compound is applicable for research in the diabetes field.

KV1.3-IN-2 (Compound I) selectively inhibits the kv1.3 potassium channel without affecting the hERG channel. It is applicable in research related to immune-associated diseases such as psoriasis, rheumatoid arthritis, and systemic lupus erythematosus.

TNF-α-IN-25 exhibits weak to moderate inhibition of the hERG-encoded potassium ion channel, with a hERG IC50 value of 9.2 μM.

DPP8/9-IN-2 (Compound 21) is an inhibitor targeting DPP8 and DPP9 with IC50 values of 0.22 nM and 3 nM, and Ki values of 2.9 nM and 6 nM, respectively. It exhibits certain cardiac toxicity, with IC50 values against the hERG potassium channel, Nav1.5 sodium channel, and Cav1.2 calcium channel of 0.7 μM, 29.0 μM, and 27.7 μM. DPP8/9-IN-2 is applicable for research into diseases such as cancer.

IDOR-1104-0086 is an orally active Kv7 potassium channel opener capable of crossing the blood-brain barrier, with an EC50 of 210 nM. It demonstrates strong selectivity for the hERG channel, with an IC20 of 25 μM. IDOR-1104-0086 exhibits efficacy and good tolerability in two rodent epilepsy models and can be utilized in epilepsy studies.

Nav1.7-IN-19 is a potent, selective, and orally active Nav1.7 inhibitor with an IC50 value of 0.49 μM. It shows high selectivity for Nav1.7, exhibiting 312-fold and 662-fold selectivity over Nav1.1 and Nav1.5, respectively, in the inactivated state. Nav1.7-IN-19 weakly inhibits the hERG potassium channel. Additionally, Nav1.7-IN-19 possesses analgesic properties, making it useful for neurological disorder research.

ASK1-IN-10 (Compound 27) is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of less than 200 nM. It also exhibits inhibitory activity on the hERG potassium channel. ASK1-IN-10 is utilized in inflammation research.