BAY 60-5521

BAY 60-5521 is an orally active cholesteryl ester transfer protein (CETP) inhibitor with an IC₅₀ of 7 nM. BAY 60-5521 inhibits CETP-mediated transfer of cholesteryl esters from HDL to LDL/VLDL, as well as the transfer of triglycerides from LDL/VLDL to HDL. It dose-dependently increases HDL-C and HDL concentrations, and slightly reduces triglyceride levels. BAY 60-5521 can be used in studies related to dyslipidemia^[1][2][3]. In Vitro:BAY 60-5521 (4-18 h) inhibits CETP activity in artificial liposome fluorescence assays, with a mean IC₅₀ of 25 nM, and a mean IC₅₀ of 7 nM measured in human lipoprotein SPA assays^[2].
BAY 60-5521 (24 h) inhibits CETP activity in human plasma and plasma from CETP transgenic mice, with mean IC₅₀ values of 50 nM and 25 nM, respectively^[2].
BAY 60-5521 potently inhibits CETP activity in cell-free CETP fluorescence buffer assays and human plasma, with IC₅₀ values of 0.025 μM and 0.05 μM, respectively^[3]. In Vivo:BAY 60-5521 inhibits CETP and increases serum HDL levels in transgenic hCETP mice^[1].
BAY 60-5521 (0.5-2 mg/kg; p.o.; single administration; 16 h-3 days) exerts CETP inhibitory activity and increases HDL-C levels in male CETP transgenic mice^[2].