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Dalcetrapib is an inhibitor of CETP that exhibits an IC50 value of 9 µM for plasma CETP in rabbits.1 Inhibition of CETP by dalcetrapib in rabbits given an atherogenic diet leads to elevation of HDL, decreased VLDL, and attenuation of the induced atherosclerosis.1 In human subjects, dalcetrapib also inhibits CETP activity and increases plasma HDL levels but it does not reduce the risk of recurrent cardiovascular events.2,3
WARNING This product is not for human or veterinary use.
1. A cholesteryl ester transfer protein inhibitor attenuates atherosclerosis in rabbits. Nature 406, 203-206 (2000).
2. Molecular regulation of HDL metabolism and function: implications for novel therapies. J. Clin. Invest. 116(12), 3090-3100 (2006).
3. Effects of dalcetrapib in patients with a recent acute coronary syndrome. N. Engl. J. Med. 367(22), 2089-2099 (2012).