BMS 182874 hydrochloride 是一种非肽内皮素 (El) 受体拮抗剂。

BMS 182874 hydrochloride is a nonpeptide endothelin (El) receptor antagonist.

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.

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.

1215703-04-0

C17H20ClN3O3S

381.88

DMSO:100mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years