Plasma phospholipid transfer protein (PLTP) is thought to play a major role in the facilitated transfer of phospholipids between lipoproteins and in the modulation of high-density lipoprotein (HDL) particle size and composition. PLTP-facilitated lipid transfer activity is related to HDL and LDL metabolism, as well as lipoprotein lipase activity, adiposity, and insulin resistance. The PLTP Drug Screening Kit utilizes rabbit serum as PLTP activity source to screen PLTP inhibitors. The assay uses a donor molecule containing a fluorescent self-quenched phospholipid that is transferred to an acceptor molecule in the presence of PLTP. PLTP-mediated transfer of the fluorescent phospholipid to the acceptor molecule results in an increase in fluorescence (Ex/ Em- 465/ 535 nm). Inhibitor of PLTP will inhibit the lipid transfer and therefore decrease fluorescence intensity. The kit provides sufficient reagents for 100 PLTP inhibitor screening assays.