CETP

Anacetrapib (MK-0859) is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease.

JTT-705 (Dalcetrapib) is a CETP inhibitor.Inhibition of CETP is a target to increase HDL-cholesterol and potentially reduce atherosclerosis.

Torcetrapib (CP-529414) is a CETP inhibitor with IC50 of 37 nM.

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. Phase 3.

CKD-519 is a selective and potent cholesteryl ester transfer protein (CETP) inhibitor being developed for the treatment of dyslipidemia to raise high-density lipoprotein cholesterol. Single doses of CKD-519 up to 400 mg were well tolerated and showed potent inhibition of CETP activity.

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.

BI-5756 is a selective CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. It promotes a significant increase in HDL-C levels while reducing LDL-C levels, thereby improving lipid profiles. Additionally, BI-5756 enhances the function of regulatory T cells and preserves T cell-mediated anti-tumor activity, exhibiting direct anti-proliferative effects on tumor cells. This compound also upregulates the expression of MHC I, MHC II, and CD80 on tumor cells and demonstrates protective effects in graft-versus-host disease. BI-5756 is applicable in research related to oncology, graft-versus-host disease, and metabolic disorders.

Obicetrapib is a potent cholesteryl ester transfer protein (CETP) inhibitor that effectively reduces atherogenic lipoproteins, including LDL-C, ApoB, and lipoprotein(a), while simultaneously increasing HDL-C levels. This compound is of significant interest in research related to dyslipidemia and atherosclerotic cardiovascular disease (ASCVD), facilitating investigations into lipid metabolism and cardiovascular health outcomes.

Obicetrapib potassium is a selective cholesteryl ester transfer protein (CETP) inhibitor that plays a crucial role in regulating lipid metabolism by modulating levels of LDL cholesterol (LDL-C), apolipoprotein B (apoB), and high-density lipoprotein cholesterol (HDL-C). This compound is valuable for research applications focused on dyslipidemia and associated cardiovascular diseases, providing insights into lipid transport mechanisms and potential therapeutic interventions.

α-Amylcinnamaldehyde serves as a ligand for the Niemann-Pick type C2 (NPC2) protein, which is crucial for cholesterol transport in various organisms. This compound is significant in the study of moth volatiles and their biological roles, potentially enhancing the understanding of lipid metabolism and transport mechanisms. Its application in research can provide insights into the molecular interactions of NPC2 and the broader implications for lipid-related disorders.

CP-532623 is a selective inhibitor of cholesteryl ester transfer protein (CETP), designed to elevate high-density lipoprotein (HDL) cholesterol levels. This compound is a close structural analogue of Torcetrapib and exhibits significant lipophilicity. CP-532623 is utilized in research exploring lipid metabolism, cardiovascular disease, and the modulation of plasma lipoprotein profiles.

MK-8262 is a potent inhibitor of cholesteryl ester transfer protein (CETP) with an IC50 of 53 nM and a log D of 5.3, indicating good oral bioavailability. This bistrifluoromethyl analogue is primarily used in research related to coronary heart disease (CHD), specifically studying the dynamics of high-density lipoprotein (HDL) and low-density lipoprotein (LDL). Its inhibition of CETP activity positions it as a valuable tool for investigating lipid metabolism and potential therapeutic approaches for cardiovascular conditions.

TAP311 is a selective inhibitor of cholesteryl ester transfer protein (CETP), exhibiting an IC50 of 62 nM. By blocking CETP activity, TAP311 effectively regulates lipid metabolism and enhances high-density lipoprotein (HDL) levels. This compound is valuable for research focused on cardiovascular disease, specifically in studies investigating the role of CETP in lipid regulation and atherosclerosis.

BMS-795311 is a potent cholesteryl ester transfer protein (CETP) inhibitor, demonstrating an IC50 of 4 nM in enzyme-based scintillation proximity assays and 0.22 μM in human whole plasma assays. This compound is utilized in research to explore lipid metabolism and its implications in cardiovascular diseases. Its oral bioavailability supports in vivo studies, making it a valuable tool in understanding CETP's role in lipid transport and potential therapeutic strategies for dyslipidemia.

CETP-IN-4 is a selective inhibitor of cholesteryl ester transfer protein (CETP), which plays a crucial role in lipid metabolism. By inhibiting CETP activity, this compound has the potential to elevate high-density lipoprotein (HDL) cholesterol levels, thereby influencing cardiovascular health. CETP-IN-4 is suitable for research applications aimed at understanding lipid metabolism disorders and developing therapeutic strategies for cardiovascular diseases.

CP-800569 is an orally active inhibitor of cholesteryl ester transfer protein (CETP). This compound has been shown to effectively reduce low-density lipoprotein levels and postprandial triglycerides while increasing high-density lipoprotein levels. CP-800569 is valuable for research focusing on metabolic diseases, providing insights into lipid metabolism and cardiovascular health.

BMS-188494 is an inhibitor of cholesteryl ester transfer protein (CETP), which plays a crucial role in lipid metabolism. This compound exhibits significant cholesterol-lowering activity by promoting the degradation of lipoproteins. BMS-188494 is utilized in research to explore its effects on lipid profiles and cardiovascular health, making it valuable for studies focused on atherosclerosis and related metabolic disorders.

Colestolone is a 15-ketosterol compound that functions as an inhibitor of both HMG-CoA reductase and cholesteryl ester transfer protein (CETP), with an in vitro IC50 value of 660 μM. This compound exhibits cholesterol-lowering properties and is valuable in researching endocrine and metabolic diseases, particularly hyperlipidemia. Its dual action on lipid metabolism makes Colestolone a significant tool for studying cholesterol regulation and associated disorders.

Obicetrapib sodium is a selective inhibitor of cholesteryl ester transfer protein (CETP). It plays a crucial role in modulating lipid metabolism and has demonstrated significant effects on increasing high-density lipoprotein (HDL) cholesterol levels. This compound is mainly utilized in research focused on atherosclerotic cardiovascular disease (ASCVD) and related lipid disorders.

DRL-17822 is a selective inhibitor of cholesteryl ester transfer protein (CETP). This compound effectively elevates high-density lipoprotein (HDL) levels, which is key in the management of type II hyperlipidemia and atherosclerotic cardiovascular disease. Notably, the bioavailability of DRL-17822 is enhanced after a high-fat meal, with improved exposure observed in the fasted state compared to its nanocrystal formulation. This makes DRL-17822 a valuable tool for research focused on lipid metabolism and cardiovascular health.

CP 524515 is a potent inhibitor of cholesteryl ester transfer protein (CETP), which contributes to the increase of high-density lipoprotein (HDL) cholesterol levels. This compound has significant implications in cardiovascular research, particularly in the study of lipid metabolism and atherosclerosis. Its ability to modulate lipid profiles makes it a valuable tool for exploring therapeutic strategies aimed at cardiovascular diseases.

Erabulenol A is a potent inhibitor of cholesteryl ester transfer protein (CETP), which plays a critical role in lipid metabolism. This compound, isolated from Penicillium sp., exhibits significant biological activity in modulating lipid levels and improving plasma HDL cholesterol levels. Erabulenol A is valuable for research applications focused on cardiovascular diseases and metabolic disorders related to cholesterol transport and homeostasis.

5-Methoxyresorcinol is a drug intermediate that mimics the chemical structure of the resorcinol-type A ring found in flavonoids, particularly catechins. This compound demonstrates low reactivity with tocopherol and exhibits minimal inhibitory effects on cholesteryl ester transfer protein (CETP). Its unique properties make it a valuable tool for research applications involving flavonoid-related biochemical studies and drug development.