Eleclazine hydrochloride (C09-1131-111)

Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC 50 value of <1 μM and approximately 14.2 μM, respectively. Eleclazine hydrochloride shows concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in porcine model. Eleclazine hydrochloride can be used to research cardiac arrhythmiasIn VitroEleclazine inhibits sodium current in hiPSC-derived cardiomyocytes with an IC 50 of 2.5 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoEleclazine (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.Form:SolidIC50& Target:Sodium current, Potassium current. Specifications and Purity: 99%. Molecular Formula: C21H17ClF3N3O3. Molecular Weight: 451.8. PubChem CID: 90479986. Isomeric SMILES: C1COC2=C(C=C(C=C2)C3=CC=C(C=C3)OC(F)(F)F)C(=O)N1CC4=NC=CC=N4.Cl.