Formulation: A solid
Formal Name: 3,4-dihydro-4-(2-pyrimidinylmethyl)-7-[4-(trifluoromethoxy)phenyl]-1,4-benzoxazepin-5(2H)-one
Purity: ≥98%
Formula Markup: C21H16F3N3O3
Formula Weight: 415,4
Shelf life (days): 1460
CAS Number: 1443211-72-0
Notes: Eleclazine is an inhibitor of the cardiac late sodium current (INa).{66240} It inhibits INa in HEK293 cells expressing the α subunit of the voltage-gated sodium channel (Nav) isoform Nav1.5 (IC50 = 0.88 µM). Eleclazine is selective for the cardiac late INa over a panel of 11 cardiac ion channels at 1 µM, as well as Nav1.1-1.4 and Nav1.6-1.8 (IC50s = ≥5 µM for all). Eleclazine reverses anemone toxin-II-induced activation of the monophasic action potential duration at 90% repolarization (MAPD90) in isolated rabbit hearts (EC50 = 0.72 µM). It inhibits S-T segment elevation in a rabbit model of cardiac ischemia-reperfusion injury induced by occlusion of the left anterior descending artery (EC50 = 0.19 µM). Eleclazine decreases the incidence of ventricular tachycardia-ventricular fibrillation and mortality in a rabbit model of ischemia-induced arrhythmia induced by left circumflex artery ligation in a dose-dependent manner.
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