1. Metabolic Enzyme/Protease
  2. CETP
  3. BMS-795311

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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BMS-795311 Chemical Structure

BMS-795311 Chemical Structure

CAS No. : 939390-99-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-795311 is a potent and orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP), with IC50s of 4 nM in an enzyme-based scintillation proximity assay (SPA) and 0.22 μM in a human whole plasma assay (hWPA), respectively[1].

IC50 & Target

IC50: 4 nM (CETP)[1]

体外研究
(In Vitro)

BMS-795311 (10 μM; 24 hours) does not increase aldosterone synthase (CYP11B2) mRNA at 10 μM in H295R cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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[1].
BMS-795311 (3-10 mg/kg; p.o. for 3 days) increases high density lipoprotein-cholesterol (HDL-C) content[1].
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[1].
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)[1].
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)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: hCETP/apoB-100 dual Tg mice[1]
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[1]
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.
分子量

671.52

Formula

C33H23F10NO3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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