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).
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
Azacosterol is a diaza derivative of cholesterol which acts as a hypocholesteremic agent by blocking delta-24-reductase causing accumulation of desmosterol. Azacosterol acts as an inhibitor of 24-dehydrocholesterol reductase (24-DHCR), preventing the formation of cholesterol from desmosterol. Although it primarily acts to inhibit 24-DHCR, the drug also inhibits other steps in cholesterol biosynthesis. The antifertility effects of the drug in birds are mediated by inhibition of steroid hormone production, steroid hormones being synthesized from cholesterol.
CP-532623, a close structural analog of Torcetrapib, is a CETP inhibitor with highly lipophilic properties. It elevates high-density lipoprotein cholesterol.
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).