herg k+

INCB 3284 is an orally available, selective and high affinity chemokine receptor 2 (CCR2) antagonist that inhibits monocyte chemotactic protein 1 from interacting with hCCR2.INCB 3284 is used in the study of hemorrhagic shock.

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.

Trk-IN-4 (PF-6683324) is a potent pan-Trk inhibitor with IC50 = 1.1~2.6 nM for TrkA TrkB TrkC and antinociceptive effects. It is also a selective type II PTK6 inhibitor with IC50 = 76 nM and has antitumor effects.

Seridopidine (ACR343) is a modulator of dopaminergic activity that is used as an oral therapy for schizophrenia, Parkinson's disease, and Tourette's syndrome.

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 hydrochloride (HT-11 hydrochloride) is a type of flavonoid.

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

Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.

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.

Betrixaban maleate is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa.

Ketanserin tartrate (KJK-945 tartrate) is a 5-HT2A receptor and α1-adrenergic receptor antagonist with antihypertensive activity, inhibits serotonin-induced vasoconstriction and platelet activation, and can be used in the study of systemic sclerosis.

Lidoflazine is a high-affinity blocker of the HERG K+ channel and is an antianginal calcium channel blocker. It carries an obvious risk of QT interval prolongation and ventricular arrhythmia.

Betrixaban (PRT054021) is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa [1]. It was selected among all lead compounds due to its low hERG channel affinity while sustaining its factor Xa inhibition capacity [3]. Betrixaban, now developed by Portola Pharmaceuticals Inc., is prescribed as a venous thromboembolism (VTE) prophylactic for adult patients with moderate to severe restricted motility or with other risks for VTE [2]. VTE can be manifested as deep vein thrombosis or pulmonary embolism and it is a leading cause of preventable death in hospitalized patients [4].

NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK KCa2 and IK KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels). It can also activate voltage-gated Kv11.1 channels (hE

Irdabisant hydrochloride (CEP-26401) is a selective, orally active, and blood-brain barrier penetrating histamine H3 receptor (H3R) inverse agonist, demonstrating high affinity with K*i values of 7.2 nM and 2.0 nM for rat and human H3R, respectively. Exhibiting relatively low hERG current inhibitory activity with an IC*50 of 13.8 μM, this compound has shown to enhance cognition and promote wakefulness in rat social recognition models, suggesting potential applications in schizophrenia or cognitive impairment research.

Protease-Activated Receptor-1 antagonist 3 is a potent antagonist of Protease-Activated Receptor-1 (IC50: 7 nM) and exhibits binding affinity to hERG K+ channels (IC50: 9 μM).

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

P-CAB agent 2 hydrochloride is a potent, orally active potassium-competitive acid blocker (P-CAB) and gastric acid secretion inhibitor. It effectively inhibits H+ K+-ATPase activity, with an IC50 value of <100 nM, and targets the hERG potassium channel with an IC50 value of 18.69 μM. Moreover, P-CAB agent 2 hydrochloride demonstrates no acute toxicity and effectively inhibits histamine-induced gastric acid secretion [1].

P-CAB Agent 2 is a potent, orally active potassium-competitive acid blocker (P-CAB) and gastric acid secretion inhibitor that effectively inhibits H+ K+-ATPase activity, showing an IC50 value of <100 nM. It also demonstrates inhibition of the hERG potassium channel with an IC50 value of 18.69 M, indicating no acute toxicity. P-CAB Agent 2 effectively curbs histamine-induced gastric acid secretion [1].

Neolinine(at 10uM) shows significant hERG K+ channel inhibition activity.

Songoramine(10 uM) demonstrates significant hERG K+ channel inhibition.

VU 0240551 is a selective antagonist of neuronal K-Cl cotransporter KCC2 inhibitor with an IC50 of 560 nM. VU 0240551 inhibits L-type calcium channels and hERG.