耗材描述
BMS-795311
产品活性: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)。
产品来源: https://www.medchemexpress.cn/bms-795311.html
研究领域:Metabolic Enzyme/Protease
作用靶点:CETP
In Vitro: BMS-795311 (10 μM; 24 hours) does not increase aldosterone synthase (CYP11B2) mRNA at 10 μM in H295R cells.
In Vivo: 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 Cmax (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).
相关产品:Evacetrapib | Anacetrapib | Dalcetrapib | Torcetrapib | CKD-519 | CP-532623 | CETP-IN-3 | CETP-IN-4 | MK-8262 | Rosenonolactone | TAP311
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