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

BMS-795311 

Cat. No.: HY-19614
Handling Instructions

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.

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BMS-795311 Chemical Structure

BMS-795311 Chemical Structure

CAS No. : 939390-99-5

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Description

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]

In Vitro

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

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].

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.
Molecular Weight

671.52

Formula

C₃₃H₂₃F₁₀NO₃

CAS No.

939390-99-5

SMILES

O=C(N[[email protected]@](C1=CC(OC(F)(F)C(F)F)=CC(F)=C1)(C2=CC=C(F)C(OC3CC3)=C2)CC4=CC=CC=C4)C5=CC=C(F)C(C(F)(F)F)=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

BMS-795311BMS795311BMS 795311CETPCholesteryl ester transfer proteincholesterylestertransferproteinSPAhWPAHDL-CantiatheroscleroticInhibitorinhibitorinhibit

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