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Cat. No. Product Name CAS No. Information


1402796-27-3 CKD-519 (Rocacetrapib, CKD519) is a potent, selective cholesteryl ester transfer protein (CETP) inhibitor, inhibits the CETP-mediated transfer of cholesteryl ester in human serum with IC50 of 2.3 nM; exhibites a maximum of 70%-86% inhibition of CETP activity and 25%-48% increase of HDL-C levels after two weeks of oral administration of 1, 3, or 10 mg/kg in transgenic mice expressing human CETP/apolipoprotein AI; CKD-519 (Rocacetrapib, CKD519) is being developed for the treatment of dyslipidemia to raise high-density lipoprotein cholesterol.


Phase 2 Clinical



939390-99-5 BMS-795311 is a potent and orally available CETP inhibitor with IC50 of 3.8 nM, inhibits cholesteryl ester (CE) transfer with IC50 of 0.22 uM; inhibits CE transfer activity at an oral dose of 1 mg/kg in human CETP/apoB-100 dual transgenic mice and increased HDL cholesterol content and size comparable to Torcetrapib in moderately-fat fed hamsters.


866399-87-3 Obicetrapib (AMG-899, TA-8995, DEX-001) is a potent, ora cholesteryl ester transfer protein (CETP) inhibitor for treatment of dyslipidaemia.


Phase 2 Clinical



1186486-62-3 Evacetrapib (LY2484595) is a potent and selective inhibitor of cholesteryl ester transfer protein (CETP) with IC50 of 5.5 nM for human recombinant CETP protein; inhibits CETP activity in human plasma with IC50 of 36 nM; shows no significant inhibition in the CEREP cell surface receptor screening, as well as the nuclear receptor panel; exhibits an ex vivo CETP inhibition ED50 of < 5 mg/kg at 8 h post oral dose and significantly elevates HDL cholesterol in vivo; Evacetrapib is a potent and selective CETP inhibitor without torcetrapib-like off-target liabilities.





875446-37-0 Anacetrapib (MK 0859) is a potent, orally active cholesteryl ester transfer protein (CETP) inhibitor with IC50 of 7.9 nM and 11.8 nM for rhCETP and C13S CETP mutant, respectively; inhibits CETP-mediated cholesterol exchange, resulting in elevated HDL-cholesterol levels and reductions in LDL-cholesterol levels, demonstrates potential to treat elevated cholesterol levels in an effort prevent cardiovascular disease.


Phase 3 Clinical



262352-17-0 Torcetrapib (CP-529414) is a potent cholesteryl ester transfer protein (CETP) inhibitor with IC50 of 37 nM; shows the potential to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease.


Phase 2 Discontinued



1149362-88-8 TAP-311 is a novel potent and selective CETP inhibitor with plasma IC50 of 62 nM; displays >170-fold selectivity over CYPs, and has excellent pharmacokinetics in rats and robust efficacy in hamsters; shows substantially reduced lipophilicity with only modest distribution into adipose tissue, and retains potency in hypertriglyceridemic plasma in vitro and in vivo; does not increase blood pressure or plasma aldosterone levels in vivo, in contrast to torcetrapib.


Phase 1 Clinical

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