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BMS 182874 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS 182874 hydrochloride图片
CAS NO:1215703-04-0
规格:98%
分子量:381.88
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
ETA antagonist
CAS:1215703-04-0
分子式:C17H19N3O3S.HCl
分子量:381.88
纯度:98%
存储:Store at -20°C

Background:

Ki: 61 nM for ETA in VSM-A10 cells; 48 nM for ETA in CHO cells


Endothelin (ET) was originally identified as a potent vasoactive substance secreted by endothelial cells that stimulated force development in isolated pig coronary arteries. ET-1 belongs to a family of highly conserved 21-amino-acid peptides produced in numerous tissues including the lung, kidney, eye, gut and central nervous system. BMS-182874 is a low molecular weight, nonpeptide endothelin (El) receptor antagonist.


In vitro: 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-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 [1].


In vivo: When administered either orally (ED50 = 30 μmol/kg) or intravenously (ED50 = 24 μmol/kg) to conscious, normotensive rats, BMS-182874 blunted the pressor response to exogenous ET-l . These data demonstrate that BMS-l 82874 is a competitive, selective and orally active ETA receptor antagonist [1].


Clinical trial: Up to now, BMS 182874 hydrochloride is still in the preclinical development stage.


Reference:
[1] MARIA L WEBB, J.  EILEEN BIRD, EDDIE C. K. LIU, PATRICIA M. ROSE, RANDY SERAFINO, PHILIP D. STEIN and SUZANNE MORELAND. BMS-182874 is a selective, nonpeptide endothelin ETA receptor antagonist. JPET 272:1124-1134, 1995.