BMS 182874 Hydrochloride

BMS 182874 HydrochlorideCAS号: 1215703-04-0分子式: C17H20ClN3O3S分子量: 381.88描述储存/保存方法可溶性/溶解性In vitro(体外研究)In vivo(体内研究)

产品描述
描述
BMS 182874 hydrochloride is a nonpeptide endothelin (El) receptor antagonist.
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:100mM
生物活性
In vitro(体外研究)
BMS-l 82874 inhibited ET-l -stimulated inositol phosphate accumulation (KB 75 nM) and calcium mobilization (Ki = 140 nM) without suppressing the maximal responses in VSM-A10 cells. BMS-182874 competitively inhibited the binding of [125I]ET-1 to ETA receptors in rat vascular smooth muscle A10 (VSM-A10) cell membranes (Ki = 61 nM) and in CHO cells stably expressing the human ETA receptor (Ki = 48 nM), but was a weak inhibitor at ETB receptors (Ki > 50 μM) and non-ET receptors.
In vivo(体内研究)
BMS-182874 blunted the pressor response to exogenous ET-l when administered either orally (ED50 = 30 μmol/kg) or intravenously (ED50 = 24 μmol/kg) to conscious, normotensive rats.