cholesteryl ester transfer protein

9(S)-HODE cholesteryl ester was originally extracted from atherosclerotic lesions. It remains uncertain whether the oxidized fatty acid portion of the molecule results from enzymatic lipoxygenation or from random lipid peroxidation. 9(S)-HODE cholesteryl ester can be used as a standard for analysis of chiral HODE cholesteryl esters.

(±)9-HODE cholesteryl ester was originally extracted from atherosclerotic lesions and shown to be produced by Cu2+-catalyzed oxidation of LDL. Later studies determined that 15-LO from rabbit reticulocytes and human monocytes were able to metabolize cholesteryl linoleate, a major component of LDL, to 9-HODE cholesteryl ester.

(±)13-HODE cholesteryl ester was originally extracted from atherosclerotic lesions and shown to be produced by Cu2+-catalyzed oxidation of LDL. Later studies determined that 15-LO from rabbit reticulocytes and human monocytes were able to metabolize cholesteryl linoleate, a major component of LDL, to 13-HODE cholesteryl ester.

9(R)-HODE cholesteryl ester was originally extracted from atherosclerotic lesions. It remains uncertain whether the oxidized fatty acid portion of the molecule results from enzymatic lipoxygenation or from random lipid peroxidation. 9(R)-HODE cholesteryl ester can be used as a standard for analysis of chiral HODE cholesteryl esters.

13(R)-HODE cholesteryl ester was originally extracted from atherosclerotic lesions. It remains uncertain whether the oxidized fatty acid portion of the molecule results from enzymatic lipoxygenation or from random lipid peroxidation. 13(R)-HODE cholesteryl ester can be used as a standard for analysis of chiral HODE cholesteryl esters.

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

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.

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).

CETP-IN-4 is a cholesteryl ester transfer protein (CETP) inhibitor.

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.

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).

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

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

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

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.

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.

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

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).

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.

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

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

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