cholesteryl ester transfer protein

CKD-519 is a selective inhibitor of cholesteryl ester transfer protein (CETP). It inhibits CETP-mediated transfer of cholesteryl ester in human serum (IC50: 2.3 nM).

Anacetrapib (MK-0859) (MK0859) is an effective, specific, reversible rhCETP and mutant CETP(C13S) inhibitor (IC50: 7.9 nM and 11.8 nM). Anacetrapib reduces the transfer of cholesteryl ester from HDL to LDL and/or VLDL thereby, producing an increase in serum HDL-cholesterol levels and a decrease in serum LDL-cholesterol levels.

Torcetrapib (CP-529414) is a cholesteryl ester transfer protein (CETP) inhibitor designed to reduce the heterotypic transfer of cholesteryl ester from HDL to LDL and/or VLDL. It failed in phase III trials due to an excess of deaths.

Dalcetrapib (RO4607381), a rhCETP inhibitor (IC50=0.2 μM), increases the plasma HDL cholesterol.

Evacetrapib (LY2484595) (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3.

Obicetrapib (AMG-899) is an inhibitor of cholesteryl ester transfer protein.

TAP311 is an inhibitor of cholesteryl ester transfer protein (CETP)(IC50 of 62 nM).

Potent cholesteryl ester transfer protein (CETP) inhibitor (IC50 = 4 nM in an enzyme-based scintillation proximity assay). Inhibits cholesteryl ester transfer and increases HDL-C levels in vivo. Orally bioavailable. Qiao et al (2015) 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)benzamid J.Med.Chem. 58 9010 PMID:26524347

MK-8262, an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor (IC 50 = 53 nM, log D = 5.3), is a bistrifluoromethyl analogue that shows promise in research related to high-density lipoprotein (HDL) and low-density lipoprotein (LDL) with potential implications for coronary heart disease (CHD).

CETP-IN-4, a cholesteryl ester transfer protein (CETP) inhibitor, effectively impedes the activity of CETP, an enzyme that facilitates the transfer of cholesteryl esters and triglycerides between lipoproteins. This inhibition may contribute to the management of dyslipidemia by altering lipid profiles and reducing cardiovascular risks. [Doses and specific effects may vary based on individual patient conditions.]

PF-04445597 is a potent, orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP).

DRL-17822 is a Cholesteryl Ester Transfer Protein (CETP) inhibitor.

Obicetrapib potassium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.

Obicetrapib calcium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.

Obicetrapib sodium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.

MK-825 is a cholesteryl ester transfer protein (CETP) inhibitor.

Stachybotramide preferentially stimulate the plasma cholesteryl ester transfer protein (CETP)-mediated transfer of cholesteryl esters (CE) from high density lipoprotein (HDL) to both very low density lipoprotein (VLDL) and low density lipoprotein (LDL).