| Identification | Back Directory | [Name]
BMS-795311
(BMS795311) | [CAS]
939390-99-5 | [Synonyms]
BMS-795311
(BMS795311)
N-[(1R)-1-[3-(Cyclopropyloxy)-4-fluorophenyl]-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide
Benzamide, N-[(1R)-1-[3-(cyclopropyloxy)-4-fluorophenyl]-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)- | [Molecular Formula]
C33H23F10NO3 | [MOL File]
939390-99-5.mol | [Molecular Weight]
671.52 |
| Hazard Information | Back Directory | [Uses]
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]. | [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 e?ect 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. |
| [storage]
Store at -20°C | [References]
[1] Jennifer XQ, et, al. Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-795311). J Med Chem. 2015 Nov 25; 58(22): 9010-26. DOI:10.1021/acs.jmedchem.5b01363 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
|