254737-87-6
254737-87-6 結(jié)構(gòu)式
基本信息
英文別名
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]-
常見問題列表
生物活性
BMS-248360 是一種高效、有口服活性的血管緊張素 II 受體 (AT1) 和內(nèi)皮素 A (ETA) 受體雙拮抗劑，對 hAT1 和 hETA 受體作用的 Ki 值分別為 10 nM 和 1.9 nM。BMS-248360 具有抗高血壓作用。靶點
Ki: 10 nM (hAT1), 1.9 nM (hETA receptor), 6.0 nM (rAT1), 1.9 nM(r ET A receptor)
體外研究
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.
體內(nèi)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 |