BMS-795311 (BMS795311)
- CAS No.
- 939390-99-5
- Chemical Name:
- BMS-795311 (BMS795311)
- 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)-
- CBNumber:
- CB34844568
- Molecular Formula:
- C33H23F10NO3
- Molecular Weight:
- 671.52
- MDL Number:
- MOL File:
- 939390-99-5.mol
BMS-795311 (BMS795311) Chemical Properties,Uses,Production
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. |
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
BMS-795311 (BMS795311) Preparation Products And Raw materials
Raw materials
Preparation Products
BMS-795311 (BMS795311) Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| TargetMol Chemicals Inc. | +8613564774135 | zijue.cai@tsbiochem.com | United States | 19905 | 58 |
| Shanghai Hongye Biotechnology Co. Ltd | 400-9205774 | sales@glpbio.cn | China | 6777 | 58 |
| BOC Sciences | -- | info@bocsci.com | USA | 0 | 65 |
| Changzhou Furuisi Biotechnology Co., Ltd | 0519-85524369 | 3477467573@qq.com | China | 8617 | 58 |
| Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 15801484223; | psaitong@jm-bio.com | China | 29772 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24875 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 5519 | 58 |
| Biosynth Biological Technology (Suzhou) Co Ltd | 51288865780 | sales@biosynth.com | China | 233051 | 58 |
| Nanjing Shizhou Biology Technology Co.,Ltd | 025-85560043 15850508050 | cindy.huang@synzest.com | China | 12000 | 58 |
View Lastest Price from BMS-795311 (BMS795311) manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-10-28 | BMS-795311
939390-99-5
|
US $1970.00-3400.00 / mg | 10g | TargetMol Chemicals Inc. |
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- BMS-795311
939390-99-5
- US $1970.00-3400.00 / mg
- TargetMol Chemicals Inc.