herg k+

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.

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.

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.

Desmethylastemizole (O-Demethylastemizole) is a metabolite of Astemizole and acts as a β-hematin (βH) inhibitor. It exhibits antimalarial activity against Plasmodium falciparum strains Pf3D7, PfDd2, and PfItG with IC50 values of 0.12 μM, 0.11 μM, and 0.06 μM, respectively. Additionally, Desmethylastemizole functions as a histamine H1 receptor antagonist and significantly blocks the hERG K+ channel while inhibiting the activity of the histone-lysine N-methyltransferase EZH2. It is utilized in studies of long QT syndrome and malaria.

Cavutilide hydrochloride (Niferidil) is a Class III antiarrhythmic agent that inhibits hERG K+ channels. Cavutilide hydrochloride holds potential for research in persistent atrial fibrillation.

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 dihydrochloride 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].

Astemizole (Standard) is a reference standard for quantitative analysis, quality control, and biochemical experiments. Astemizole (Laridal) is a long-acting, non-sedating antihistamine. It acts as a histamine H1 receptor antagonist (IC50 = 4 nM) and an hERG K+ channel blocker (IC50 = 0.9 nM), exhibiting anticholinergic and antipruritic effects. It is indicated for inflammatory conditions such as rhinitis and asthma.

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