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IC50: 6 μM for CETP inhibition in human plasma

Cholesteryl ester transfer protein (CETP) is a plasma protein that transfers neutral lipids among the lipoproteins. Its most important action is the exchange of cholesteryl esters in high-density lipoprotein (HDL) for triglycerides in very low-density lipoprotein. Thus, CETP is a potentially atherogenic protein, and its atherogenicity has been supported by many studies. Dalcetrapib is a novel inhibitors of CETP.

In vitro: Dalcetrapib achieved 50% inhibition of CETP activity in human plasma at a concentration of 6 μM. The mechanism of action was considered to involve the formation of a disulfide bond between the thiol form of Dalcetrapib and the cysteine residue at position 13 (Cys13) of CETP. [1].

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