Cholesteryl ester transfer protein (CETP) is a plasma protein that transfers a cholesteryl ester from HDL to LDL or VLDL in exchange for a triglyceride. HDL plays an important role in lipid metabolism and cardiovascular health. HDL transports cholesterol to the liver for excretion or to steroidogenic tissues for steroid synthesis. HDL also plays an important role in the reverse cholesterol transport pathway, removing cholesterol from lipid-filled macrophages, protecting against atherosclerosis. Because of this function, CETP is viewed as a target to increase HDL, with CETP inhibition an active area of research and several CETP inhibitors at various stages of drug development. Assay Genie's CETP Activity Fluorometric Assay Kit uses a self-quenched fluorescent neutral lipid that can be measured when transferred to an acceptor molecule. The fluorometric intensity is directly proportional to the amount of neutral lipid transfer. Rabbit serum is provided as a positive control and CETP inhibitor Torcetrapib is included for assay validation. This Assay Kit, in addition to measuring activity in serum, is also suitable for testing activity of recombinant protein.

Figure: (a) Donor Molecule Standard Curve, (b) Measurement of CETP activity of rabbit serum (1 µl), human plasma (1 µl) or recombinant human CETP (800 ng) (Cat # 7606), (c) Inhibition of CETP activity from rabbit serum by Torcetrapib. The assay was run for 1 hr and the IC50 was determined to be 3.56 nM and (d) Inhibition of CETP activity from human plasma using 80 nM Torcetrapib, assay was run for 2 hrs.