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254737-87-6

中文名稱 BMS-248360
CAS 254737-87-6
分子式 C36H45N5O5S
分子量 659.84
MOL 文件 254737-87-6.mol
254737-87-6 結(jié)構(gòu)式 254737-87-6 結(jié)構(gòu)式

基本信息

英文別名
BMS-248360
BMS-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(wèn)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(duì) 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(diǎn)

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
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