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Description: Eleclazine hydrochloride (also known as GS-6615) is a novel late Na+ current inhibitor with IC50 value of 0.7 uM. Enhanced late Na+ current (late INa ) in the myocardium is pro-arrhythmic. Inhibition of this current is a promising strategy to stabilize ventricular repolarization and suppress arrhythmias. Eleclazine was a selective inhibitor of late INa , stabilizes the ventricular repolarization and suppresses arrhythmias in a model of LQT3. The concentrations at which the electrophysiological effects of Eleclazine were observed are comparable to plasma levels associated with QTc shortening in patients with LQT3, indicating that these effects are clinically relevant. Eleclazine is currently in clinical development for the treatment of long QT syndrome 3 (LQT3).
References: Br J Pharmacol. 2016 Nov; 173(21):3088-3098; Heart Rhythm. 2016 Sep; 13(9):1860-7.
Related CAS#: 1443211-72-0 (free base)
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