254737-87-6
254737-87-6 结构式
基本信息
中文别名
化合物 T14672化合物 BMS-248360
英文别名
BMS-248360BMS-248360 >=98% (HPLC)
[1,1'-Biphenyl]-2-sulfonamide, 4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-N-(3,4-dimethyl-5-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-
常见问题列表
生物活性
BMS-248360 是一种高效、有口服活性的血管紧张素 II 受体 (AT1) 和内皮素 A (ETA) 受体双拮抗剂，对 hAT1 和 hETA 受体作用的 Ki 值分别为 10 nM 和 1.9 nM。BMS-248360 具有抗高血压作用。靶点
Ki: 10 nM (hAT1), 1.9 nM (hETA receptor), 6.0 nM (rAT1), 1.9 nM(r ET A receptor)
体外研究
BMS-248360 shows activity against rat AT1 and rat ET
A
receptor, with K
i
s of 6.0 nM and 1.9 nM, respectively.
BMS-248360 shows no activity against AT2 and ET
B
receptor subtypes.
体内研究
BMS-248360 is found to be orally bioavailable in rats (%F=38) with excellent oral exposure (C
max
)=3.1 µM) and reasonable elimination profile (T
1/2
=5.5 hours).
BMS-248360 (30 µmol/kg, 100 µmol/kg; p.o.) blocks the hypertensive effects of intravenously administered AII.
| Animal Model: | Male Rats |
| Dosage: | 30 µM/kg, 100 µM/kg |
| Administration: | Oral administration |
| Result: | Blocked the hypertensive effects of intravenously administered AII. |
| Animal Model: | Male Rats |
| Dosage: | 10 µM/kg |
| Administration: | Oral administration |
| Result: | T 1/2 = 5.5 hours |