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BMS-795311  

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包装规格：1mg in glass bottle
产品描述：基本信息 产品编号： B11363 产品名称： BMS-795311 CAS: 939390-99-5   储存条件 粉末 -20℃ 四年     分子式： C33H23F10NO3 溶于液体     分子量 671.52     化学名：  N-[(1R)-1-(3-Cyclopropyloxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide   生物活性 产品描述 一种有效的，具有口服活性的胆固醇酯转移蛋白CETP抑制剂 靶点 IC50: 4nM (CETP) 体外研究 BMS-795311 (10μM; 24 hours) does not increase aldosterone synthase (CYP11B2) mRNA at 10μM in H295R cells 体内研究 BMS-795311 (1-3mg/kg; oral administration) inhibits plasma CE transfer activity in human CETP (hCETP)/apoB-100 dual transgenic (Tg) mice. BMS-795311 (3-10mg/kg; p.o. for 3 days) increases high density lipoprotein-cholesterol (HDL-C) content. BMS-795311 (8mg/kg, i.v.) has no effect 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 Cmax (mice 5.3, rats 17, monkeys 1.7, dogs 0.43 ng/mL) following oral administration (mice 10, rats 10, monkeys 5, dogs 5mg/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 1mg/kg) Animal Model: hCETP/apoB-100 dual Tg mice Dosage:  1, 3mg/kg Administration: Oral administration Result: Inhibited CETP activity at a dose of 1mg/kg at the 8 h time point.   Animal Model: Moderately fat-fed hamsters Dosage: 3, 10mg/kg Administration: Oral administration for 3 days Result: Increased plasma high density lipoprotein-cholesterol (HDL-C) content by 45% when dosed at 10mg/kg.
保存条件：-20℃

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