Eleclazine

Eleclazine is an inhibitor of the cardiac late sodium current (INa). It inhibits INa in HEK293 cells expressing the alpha 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.Formal Name: 3,4-dihydro-4-(2-pyrimidinylmethyl)-7-[4-(trifluoromethoxy)phenyl]-1,4-benzoxazepin-5(2H)-one. CAS Number: 1443211-72-0. Synonyms: Dihydrobenzoxazepinone, GS-6615. Molecular Formula: C21H16F3N3O3. Formula Weight: 415.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 20 mg/ml, DMSO: 12 mg/ml, Ethanol: 5 mg/ml, PBS (pH 7.2): 0.16 mg/ml. lambdamax: 248 nm. SMILES: O=C1C2=CC(C3=CC=C(OC(F)(F)F)C=C3)=CC=C2OCCN1CC4=NC=CC=N4. InChi Code: InChI=1S/C21H16F3N3O3/c22-21(23,24)30-16-5-2-14(3-6-16)15-4-7-18-17(12-15)20(28)27(10-11-29-18)13-19-25-8-1-9-26-19/h1-9,12H,10-11,13H2. InChi Key: YNUAEEJQYHYLMS-UHFFFAOYSA-N.