T45587 |
BMS 182874 Hydrochloride |
源叶(MedMol) | 98% |
- 产品描述: BMS 182874 hydrochloride is a nonpeptide endothelin (El) receptor antagonist.
- 靶点: Endothelin Receptor;EndothelinReceptor
- 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
- 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.
- 参考文献:
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.
- 溶解性: Soluble in DMSO
- 保存条件: 2-8°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.619 ml 13.093 ml 26.186 ml 5 mM 0.524 ml 2.619 ml 5.237 ml 10 mM 0.262 ml 1.309 ml 2.619 ml 50 mM 0.052 ml 0.262 ml 0.524 ml
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