cetp

Anacetrapib (MK-0859) 是 CETP 的抑制剂，能够抑制 rhCETP (IC50:7.9±2.5 nM) 和 C13S CETP 突变型 (IC50:11.8±1.9 nM) 的活性。

TAP311 is an inhibitor of cholesteryl ester transfer protein (CETP)(IC50 of 62 nM).

CP-532623, a close structural analog of Torcetrapib, is a CETP inhibitor with highly lipophilic properties. It elevates high-density lipoprotein cholesterol.

是胆固醇酯转移蛋白 (CETP) 选择性抑制剂。根据人血浆的抑制曲线，Torcetrapib (CP-529414) 对CETP 的最有效浓度为 37 nM。

Dalcetrapib (RO4607381) 是rhCETP 抑制剂(IC50:0.2 μM)，具有增加血浆中HDL 胆固醇含量的作用。

CETP-IN-3 is an inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP.

CETP-IN-4 is a cholesteryl ester transfer protein (CETP) inhibitor.

Obicetrapib (AMG-899) 是胆固醇酯转移蛋白的抑制剂。

Evacetrapib (LY2484595) 是 CETP 的选择性抑制剂，在人血浆中，抑制人重组 CETP 蛋白 (IC50:5.5 nM) 和 CETP (IC50:36 nM) 活性。

Dirlotapide (CP742033) 是一种肠道选择性微粒体甘油三酯转移蛋白(MTP)抑制剂。它可以减轻糖尿病狗的体重。Dirlotapide 以剂量依赖性方式减少食物摄入量，可能是通过增加 肽YY 释放到循环中。

CP 524515 是一种胆固醇酯转移蛋白 (CETP) 的有效抑制剂，能够增加高密度脂蛋白胆固醇水平。

20-HC-Me-Pyrrolidine是一种有效的Aster蛋白抑制剂，对 Aster-A、Aster-B 和 Aster-C 的 IC50=0.06~0.71 μm，能够阻断Aster蛋白结合和转移胆固醇的能力，包括抑制LDL胆固醇向内质网的移动。

Campesterol ((24R)-5-Ergosten-3β-ol) 是一种植物甾醇，具有降胆固醇和抗癌的活性。

BMS-212122 (UNII-0Z473OO6GB) 是一种有效的微粒体甘油三酯转移蛋白(MTP )抑制剂，在动物实验中显示出降血脂作用。BMS-212122 显著减少动脉粥样硬化斑块中的脂质含量和单核细胞衍生(CD68+)细胞。

Granotapide 是一种微粒体甘油三酯转移蛋白（MTP）抑制剂，治疗和而预防动脉硬化，冠状动脉疾病，代谢综合征，肥胖，糖尿病，糖尿病前期和高血压。

Lomitapide (AEGR-733) 是一种高效的微粒体甘油三酯转移蛋白(MTP)抑制剂，体内试验的IC50值为8 nM。

KD-026 (SLx 4090) 是具有口服活性的、肠细胞特异性的微粒体甘油三酯转移蛋白 (MTP)抑制剂，IC50为 8.0 nM。KD-026 (SLx 4090) 在糖尿病2型中有研究的价值。

Lomitapide Mesylate (BMS-201038 mesylate) 是一种高效MTP 蛋白抑制剂，其体外IC50值为8 nM。

Implitapide is an inhibitor of microsomal triglyceride transfer protein (MTP).

CKD-519 is a selective inhibitor of cholesteryl ester transfer protein (CETP). It inhibits CETP-mediated transfer of cholesteryl ester in human serum (IC50: 2.3 nM).

MK-825盐酸半乙酸乙酯是一种CETP抑制剂。

BAY-60-5521 is an effective cholesterol ester transfer protein (CETP) inhibitor.

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.

Potent cholesteryl ester transfer protein (CETP) inhibitor (IC50 = 4 nM in an enzyme-based scintillation proximity assay). Inhibits cholesteryl ester transfer and increases HDL-C levels in vivo. Orally bioavailable. Qiao et al (2015) Triphenylethanamine derivatives as cholesteryl ester transfer protein inhibitors: discovery of N-[(1R)-1-(3-cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamid J.Med.Chem. 58 9010 PMID:26524347