BMS 795311
- CAS号:939390-99-5
- 英文名:BMS-795311 (BMS795311)
- 中文名:BMS 795311
- CBNumber:CB34844568
- 分子式:C33H23F10NO3
- 分子量:671.52
- MOL File:939390-99-5.mol
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
BMS 795311性质、用途与生产工艺
- 生物活性 BMS-795311 是一种有效的，具有口服活性的胆固醇酯转移蛋白 CETP 抑制剂， IC50 值分别为 4 nM (SPA) 和 0.22 μM (hWPA)。
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靶点
IC50: 4 nM (CETP)
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体外研究
BMS-795311 (10 μM; 24 hours) does not increase aldosterone synthase (CYP11B2) mRNA at 10 μM in H295R cells.
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体内研究
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 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 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.
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5729
- 优势度：77
