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Anacetrapib is an inhibitor of cholesterol ester transfer protein (CETP) with IC50 values of 17 and 15 nM for CETP-dependent transfer of cholesterol esters and triglycerides, respectively.1 It decreases plasma levels of LDL and triglycerides, reduces atherosclerotic lesion sizes, and increases HDL levels in the E3L.CETP mouse model of atherosclerosis.2 Anacetrapib (150 mg/kg) increases HDL levels by 2-fold and lowers LDL and fasting plasma triglyceride levels in rhesus macaques.3
WARNING This product is not for human or veterinary use.
1. Biochemical characterization of cholesteryl ester transfer protein inhibitors. J. Lipid. Res. 51(9), 2739-2752 (2010).
2. Anacetrapib reduces (V)LDL cholesterol by inhibition of CETP activity and reduction of plasma PCSK9. J. Lipid Res. 56(11), 2085-2093 (2015).
3. Evaluation of CETP activity in vivo under non-