CAS NO: | 939390-99-5 |
规格: | ≥98% |
BMS-795311 is a potent CETP inhibitor that maximally inhibited cholesteryl ester (CE) transfer activity at an orally bioavailable dose of 1 mg/kg in human ETP/apoB-100 dual transgenic mice and increased HDL cholesterol content and size comparable to torcetrapib in moderately-fat fed hamsters. Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that is responsible for transporting neutral lipids such as cholesteryl esters (CEs) and triglycerides (TGs) among various classes of lipoproteins including HDL, LDL, and very low density lipoprotein (VLDL).2 Physiologically, CETP facilitates the transfer of CE from HDL to LDL and VLDL in exchange for TG, leading to decreased HDL-C levels and increased LDL-C levels. References: Qiao JX, Wang TC, Adam LP, Chen AY, Taylor DS, Yang RZ, Zhuang S, Sleph PG, Li JP, Li D, Yin X, Chang M, Chen XQ, Shen H, Li J, Smith D, Wu DR, Leith L, Harikrishnan LS, Kamau MG, Miller MM, Bilder D, Rampulla R, Li YX, Xu C, Lawrence RM, Poss MA, Levesque P, Gordon DA, Huang CS, Finlay HJ, Wexler RR, Salvati ME. 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 17. [Epub ahead of print] PubMed PMID: 26524347.
纯度:≥98%
CAS:939390-99-5
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