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编 号:F166696
分子式:C21H17ClF3N3O3
分子量:451.83
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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生物活性:
Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC50 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 arrhythmias.

体内研究:
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.

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