Eleclazine hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型、强效、选择性的晚钠电流 (late INa) 抑制剂，用于治疗长 QT-3 综合征 (LQT-3)。

A novel, potent, and selective inhibitor of Late sodium current (late INa) for treatment of long QT-3 syndrome (LQT-3), hypertrophic cardiomyopathy (HCM), and ventricular tachycardia–ventricular fibrillation (VT–VF); 42 times more potent than Ranolazine in reducing ischemic burden in vivo (EC50=190 nM).Heart Arrhythmia Phase 3 Clinical(In Vitro):Eleclazine inhibits sodium current in hiPSC-derived cardiomyocytes with an IC50 of 2.5 μM.(In Vivo):Eleclazine (0.3 and 0.9 mg/kg; IV; infused over 15 minutes) reduces the incidence of epinephrine-induced ventricular premature beats and couplets, and shortens ventricular QT and atrial PTa intervals.

Eleclazine inhibits sodium current in hiPSC-derived cardiomyocytes with an IC50 of 2.5 μM.

Eleclazine (0.3 and 0.9 mg/kg; IV; infused over 15 minutes) reduces the incidence of epinephrine-induced ventricular premature beats and couplets, and shortens ventricular QT and atrial PTa intervals. Animal Model:Male Yorkshire pigs (35.20 ± 0.46 kg; injected with epinephrine via a jugular vein)Dosage:0.3 and 0.9 mg/kg Administration:IV; infused over 15 minutes Result:Reduced the incidence of epinephrine-induced ventricular premature beats and couplets by 51% (from 31.3 ± 1.91 to 15.2 ± 5.08 episodes; P = 0.038) and the incidence of 3- to 7-beat ventricular tachycardia (VT) by 56% (from 10.8 ± 3.45 to 4.7 ± 3.12 episodes; P = 0.004).Shortened ventricular QT and atrial PTa intervals by 7%, and reduced atrial repolarization alternans and heterogeneity without attenuation of the inotropic response to catecholamine.

GS-6615 hydrochloride

Membrane Transporter/Ion Channel

Sodium Channel

Sodium Channel

Cardiovascular Disease

Heart Arrhythmia

1448754-43-5

451.8262

C21H17ClF3N3O3

>98% (HPLC)

10 mM in DMSO

O=C1N(CC2=NC=CC=N2)CCOC3=CC=C(C4=CC=C(OC(F)(F)F)C=C4)C=C13.[H]Cl

1,4-Benzoxazepin-5(2H)-one, 3,4-dihydro-4-(2-pyrimidinylmethyl)-7-[4-(trifluoromethoxy)phenyl]-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years