1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. CETP

CETP

Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that facilitates the transfer of cholesteryl esters from the atheroprotective high density lipoprotein (HDL) to the proatherogenic low density lipoprotein cholesterol (LDL) and very low density lipoprotein cholesterol (VLDL) leading to lower levels of HDL but raising the levels of proatherogenic LDL and VLDL. CETP inhibitors are a class of drugs that targets the CETP enzyme to significantly increase serum HDL-C and decrease LDL-C levels. Inhibition of CETP is considered a potential approach to treat dyslipidemia.

Alterations of CETP activity levels can be caused by single-base polymorphisms as well as by alternative splicing. Several common variants in CETP have been reported to be associated with variation in plasma lipid levels, CAD risk and/or CETP mass/activity. The rare genetic variants in the CETP gene also contribute to the phenotypic variation of HDL-C in the general population.

CETP Related Products (10):

Cat. No. Product Name Effect Purity
  • HY-12090
    Anacetrapib
    Inhibitor 99.62%
    Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively.
  • HY-12089
    Torcetrapib
    Inhibitor 99.39%
    Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM.
  • HY-13327
    Evacetrapib
    Inhibitor ≥98.0%
    Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
  • HY-14950
    Dalcetrapib
    Inhibitor 99.42%
    Dalcetrapib (JTT-705; RO-4607381) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol.
  • HY-116078
    CKD-519
    Inhibitor
    CKD-519 is a selective and potent cholesteryl ester transfer protein (CETP) inhibitor, which inhibits CETP-mediated transfer of cholesteryl ester in human serum with an IC50 of 2.3 nM.
  • HY-132303
    MK-8262
    Inhibitor
    MK-8262 is an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 53 nM and a log D of 5.3. MK-8262, a bistrifluoromethyl analogue, has the potential for coronary heart disease (CHD) correlated high-density lipoprotein (HDL) and low-density lipoprotein (LDL) research.
  • HY-107997
    TAP311
    Inhibitor
    TAP311 is a cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 62 nM.
  • HY-128338
    CETP-IN-3
    Inhibitor
    CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitory activity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC50s of 0.002 μM and 0.06 μM, respectively.
  • HY-19614
    BMS-795311
    Inhibitor
    BMS-795311 is a potent and orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP), with IC50s of 4 nM in an enzyme-based scintillation proximity assay (SPA) and 0.22 μM in a human whole plasma assay (hWPA), respectively.
  • HY-123039
    CP-532623
    Inhibitor ≥99.0%
    CP-532623 is a CETP inhibitor and elevates high-density lipoprotein cholesterolion. CP-532623 is a close structural analogue of Torcetrapib. CP-532623 has highly lipophilic properties.
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