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Eleclazine hydrochloride

  Cat. No.:  DC22533   Featured
Chemical Structure
1448754-43-5
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More than 5000 active chemicals with high quality for research!
Field of application
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).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1448754-43-5
Chemical Name: 1,4-Benzoxazepin-5(2H)-one, 3,4-dihydro-4-(2-pyrimidinylmethyl)-7-[4-(trifluoromethoxy)phenyl]-, hydrochloride (1:1)
Synonyms: GS-6615 hydrochloride
SMILES: O=C1C2C(=CC=C(C=2)C2C=CC(OC(F)(F)F)=CC=2)OCCN1CC1N=CC=CN=1.[H]Cl
Formula: C21H17ClF3N3O3
M.Wt: 451.8262
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Eleclazine hydrochloride is a novel late Na+ current inhibitor with IC50 value of 0.7 uM. target: Na+ current.
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]
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
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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