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.
货号 | 产品名 | Cas | 产品描述 |
---|---|---|---|
PL02479 | Anacetrapib | 875446-37-0 | Anacetrapib 是一种有效的 CETP 抑制剂,作用于 rhCETP 和 C13S CETP 突变型,IC50 分别为 7.9±2.5 nM 和 11.8±1.9 nM。 |
PL02588 | CP-532623 | 261947-38-0 | CP-532623 是 CETP 抑制剂,可提高高密度脂蛋白胆固醇水平。CP-532623 与 Torcetrapib 的结构相似,并具有高度亲脂性。 |
PL04308 | Dalcetrapib | 211513-37-0 | Dalcetrapib (JTT-705) 是一种具有口服活性的胆固醇酯转运蛋白 (CETP) 抑制剂,对 rhCETP 和人血浆 CETP 的 IC50 分别为 204.6 nM 和 6 μM。 |
PC12523 | Evacetrapib (LY2484595) | 1186486-62-3 | 强效的CETP选择性抑制剂,Evacetrapib 是一种有效的选择性的 CETP 抑制剂,在人血浆中,抑制人重组 CETP 蛋白 (IC50 为 5.5 nM) 和 CETP 活性,IC50 为 36 nM。 |
PC12524 | Torcetrapib | 262352-17-0 | CETP抑制剂,Torcetrapib(CP-529414)是CETP高效抑制剂,IC50值为37nM。 |