Signaling Pathway

CETP

CETP

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CETP (Cholesteryl ester transfer protein ) is a plasma protein that facilitates the transport ofcholesteryl esters and triglycerides between the lipoproteins. It collects triglycerides from very-low-density (VLDL) or low-density lipoproteins (LDL) and exchanges them for cholesteryl esters from high-density lipoproteins (HDL), and vice versa. Most of the time, however, CETP does a hetero exchange, trading a triglyceride for a cholesteryl ester or a cholesteryl ester for a triglyceride. Rare mutations leading to increased function of CETP have been linked to accelerated atherosclerosis. A CETP inhibitor is a member of a class of drugs that inhibit cholesterylester transfer protein (CETP). They are intended to reduce the risk of atherosclerosis (a cardiovascular disease) by improving blood lipid levels. This category of drugs substantially increases HDL and reverse cholesterol transport.

CETP Inhibitors & Modulators (4)

Product Name Catalog No. Brief Description
Anacetrapib

HY-12090

Anacetrapib (MK0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure.

Dalcetrapib

HY-14950

Dalcetrapib (JTT-705; RO-4607381) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol.

Evacetrapib

HY-13327

Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure.

Torcetrapib

HY-12089

Torcetrapib(CP-529414) is a CETP inhibitor with IC50 of 37 nM, elevates HDL-C and reduces nonHDL-C in plasma.