BMS-795311

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMS-795311 是一种有效的口服 CETP 抑制剂，IC50 为 3.8 nM，抑制胆固醇酯 (CE) 转移，IC50 为 0.22 uM。

BMS-795311 is a potent and orally available CETP inhibitor with IC50 of 3.8 nM, inhibits cholesteryl ester (CE) transfer with IC50 of 0.22 uM; inhibits CE transfer activity at an oral dose of 1 mg/kg in human CETP/apoB-100 dual transgenic mice and increased HDL cholesterol content and size comparable to Torcetrapib in moderately-fat fed hamsters.

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

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 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). 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.

BMS795311

Metabolic Enzyme/Protease

CETP

CETP

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939390-99-5

671.535

C33H23F10NO3

>98% (HPLC)

——

C1CC1OC2=C(C=CC(=C2)C(CC3=CC=CC=C3)(C4=CC(=CC(=C4)F)OC(C(F)F)(F)F)NC(=O)C5=CC(=C(C=C5)F)C(F)(F)F)F

N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide

(-20℃)

With Ice Pack

≥ 2 years