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939390-99-5

中文名稱 BMS 795311
英文名稱 BMS-795311 (BMS795311)
CAS 939390-99-5
分子式 C33H23F10NO3
分子量 671.52
MOL 文件 939390-99-5.mol
939390-99-5 結(jié)構(gòu)式 939390-99-5 結(jié)構(gòu)式

基本信息

英文別名
BMS-795311 (BMS795311)
N-[(1R)-1-[3-(Cyclopropyloxy)-4-fluorophenyl]-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide
Benzamide, N-[(1R)-1-[3-(cyclopropyloxy)-4-fluorophenyl]-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)-

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度溶于二甲基亞砜

常見問題列表

生物活性
BMS-795311 是一種有效的,具有口服活性的膽固醇酯轉(zhuǎn)移蛋白 CETP 抑制劑, IC50 值分別為 4 nM (SPA) 和 0.22 μM (hWPA)。
靶點(diǎn)

IC50: 4 nM (CETP)

體外研究

BMS-795311 (10 μM; 24 hours) does not increase aldosterone synthase (CYP11B2) mRNA at 10 μM in H295R cells.

體內(nèi)研究

BMS-795311 (1-3 mg/kg; oral administration) inhibits plasma CE transfer activity in human CETP (hCETP)/apoB-100 dual transgenic (Tg) mice.
BMS-795311 (3-10 mg/kg; p.o. for 3 days) increases high density lipoprotein-cholesterol (HDL-C) content.
BMS-795311 (8 mg/kg, i.v.) has no e?ect on mean, systolic, or diastolic blood pressure, heart rate, or locomotor activity in rat telemetry studies.
BMS-795311 exhibits reasonable oral bioavailability (mice 37%, rats 37%, monkeys 20%, dogs 5%) and C max (mice 5.3, rats 17, monkeys 1.7, dogs 0.43 ng/mL) following oral administration (mice 10, rats 10, monkeys 5, dogs 5 mg/kg).
BMS-795311 exhibits terminal elimination half-lives (mice 6, rats 7, monkeys >18, dogs 10 h) due to low plasma clearance (2.0, 0.9, 0.9, and 1.4 mL/min/kg respectively) combined with little volumes of distribution (0.8, 0.4, 0.9, and 0.6 L/kg respectively) following intravenous administration (mice 5, rats 1, monkeys 4, dogs 1 mg/kg).

Animal Model: hCETP/apoB-100 dual Tg mice
Dosage: 1, 3 mg/kg
Administration: Oral administration
Result: Inhibited CETP activity at a dose of 1 mg/kg at the 8 h time point.
Animal Model: Moderately fat-fed hamsters
Dosage: 3, 10 mg/kg
Administration: Oral administration for 3 days
Result: Increased plasma high density lipoprotein-cholesterol (HDL-C) content by 45% when dosed at 10 mg/kg.
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