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.
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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.
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基本信息 | |
可溶性/溶解性 |
DMSO:100mM
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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.
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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.
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