1448754-43-5

1448754-43-5 structure

Name: Eleclazine hydrochloride
Chemical Name: Eleclazine hydrochloride
CAS Number: 1448754-43-5
Molecular Formula: C₂₁H₁₇ClF₃N₃O₃
Molecular Weight: 451.826
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
Create Date: 2018-02-24 12:31:27
Modify Date: 2024-01-02 16:34:27
Eleclazine hydrochloride is a novel late Na+ current inhibitor with IC50 value of 0.7 uM. target: Na+ current.IC50: 0.7 uM.In vitro: Eleclazine hydrochloride inhibits ATX-II enhanced late INa in ventricular myocytes, shorten the ATX-II induced prolongation of APD, MAPD, QT interval, and decreased spatiotemporal dispersion of repolarization and ventricular arrhythmias. Inhibition by GS-6615 of ATX-II enhanced late INa is strongly correlated with shortening of myocyte APD and isolated heart MAPD[1]. Selective inhibition of cardiac late INa with eleclazine hydrochloride confers dual protection against vulnerability to ischemia-induced AF and reduces atrial and ventricular repolarization abnormalities before and during adrenergic stimulation without negative inotropic effects. [2]

Name	Eleclazine hydrochloride
Synonyms	1,4-Benzoxazepin-5(2H)-one, 3,4-dihydro-4-(2-pyrimidinylmethyl)-7-[4-(trifluoromethoxy)phenyl]-, hydrochloride (1:1) 4-(2-Pyrimidinylmethyl)-7-[4-(trifluoromethoxy)phenyl]-3,4-dihydro-1,4-benzoxazepin-5(2H)-one hydrochloride (1:1) 4R1JP3Q4HI ELECLAZINE HYDROCHLORIDE Eleclazine (hydrochloride)

Description	Eleclazine hydrochloride is a novel late Na+ current inhibitor with IC50 value of 0.7 uM. target: Na+ current.IC50: 0.7 uM.In vitro: Eleclazine hydrochloride inhibits ATX-II enhanced late INa in ventricular myocytes, shorten the ATX-II induced prolongation of APD, MAPD, QT interval, and decreased spatiotemporal dispersion of repolarization and ventricular arrhythmias. Inhibition by GS-6615 of ATX-II enhanced late INa is strongly correlated with shortening of myocyte APD and isolated heart MAPD[1]. Selective inhibition of cardiac late INa with eleclazine hydrochloride confers dual protection against vulnerability to ischemia-induced AF and reduces atrial and ventricular repolarization abnormalities before and during adrenergic stimulation without negative inotropic effects. [2]
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel Research Areas >> Others
References	[1]. Rajamani S et al. The novel late Na+ current inhibitor, GS-6615 (eleclazine) and its anti-arrhythmic effects in rabbit isolated heart preparations. Br J Pharmacol. 2016 Jul 23. [2]. Justo F et al. Inhibition of the cardiac late sodium current with eleclazine protects against ischemia-induced vulnerability to atrial fibrillation and reduces atrial and ventricular repolarization abnormalities in the absence and presence of concurrent a