CETP Inhibitor

20-HC-Me-Pyrrolidine (compound AI-3d) is a potent Aster protein inhibitor with IC₅₀s of 0.11 μM, 0.06 μM, and 0.71 μM for Aster-A, Aster-B, and Aster-C, respectively. 20-HC-Me-Pyrrolidine blocks the ability of Asters to bind and transfer cholesterol. 20-HC-Me-Pyrrolidine also inhibits the movement of low-density lipoprotein (LDL) cholesterol to the endoplasmic reticulum (ER).

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.

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.

Obicetrapib (TA-8995; DEZ-001) is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib potently reduces atherogenic lipoproteins (such as LDL-C, ApoB, Lp (a)) and increases HDL-C. Obicetrapib can be used for the research of dyslipidemia and atherosclerotic cardiovascular disease (ASCVD).

Dalcetrapib (JTT-705) is an orally active cholesteryl ester transfer protein (CETP) inhibitor with IC₅₀s of 204.6 nM and 6 μM against recombinant human (rh) CETP and human plasma CETP, respectively.

Azalanstat (RS-21607) is an orally active lanosterol 14α-demethylase inhibitor. Azalanstat exerts a cholesterol-lowering effect by inhibiting cholesterol synthesis and regulating HMG-CoA Reductase (HMGCR), and shows an additive effect when used in combination with Cholestyramine (HY-104081). Azalanstat is used in the study of hypercholesterolemia.

UBA6-IN-1 is a UBA6/UBE1L2 inhibitor (IC₅₀ ≤50 nM) that acts by reducing the level of squalene epoxidase (SQLE). UBA6-IN-1 affects SREBP-dependent lipid metabolism processes and downstream cholesteryl ester transport, and can be used for cancer research.

BAY 60-5521 is an orally active cholesteryl ester transfer protein (CETP) inhibitor with an IC₅₀ of 7 nM. BAY 60-5521 inhibits CETP-mediated transfer of cholesteryl esters from HDL to LDL/VLDL, as well as the transfer of triglycerides from LDL/VLDL to HDL. It dose-dependently increases HDL-C and HDL concentrations, and slightly reduces triglyceride levels. BAY 60-5521 can be used in studies related to dyslipidemia.

3-Pyridinemethanol (Nicotinyl alcohol), a pyridine derivative, is a cholesterol-lowering agent. 3-Pyridinemethanol can be selectively oxidized to vitamin B3.

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.

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.

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.

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

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.

Rosenonolactone shows inhibitory activity against prolyl endopeptidase and thrombin and cholesterol ester transfer protein.

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.

Obicetrapib (TA-8995; DEZ-001) potassium is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib potassium potently reduces atherogenic lipoproteins (such as LDL-C, ApoB, Lp (a)) and increases HDL-C. Obicetrapib potassium can be used for the research of dyslipidemia and atherosclerotic cardiovascular disease (ASCVD).

Azalanstat (RS-21607) dihydrochloride is an orally active lanosterol 14α-demethylase inhibitor. Azalanstat dihydrochloride exerts a cholesterol-lowering effect by inhibiting cholesterol synthesis and regulating HMG-CoA Reductase (HMGCR), and shows an additive effect when used in combination with Cholestyramine (HY-104081). Azalanstat dihydrochloride is used in the study of hypercholesterolemia.

Tiqueside (CP‐88,818) is an orally active cholesterol absorption inhibitor. Tiqueside inhibits absorption of both dietary cholesterol and endogenous cholesterol excreted into the intestinal lumen via the bile. Tiqueside can be used in the research of hypercholesterolemia.

BI-5756 is a CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. BI-5756 can significantly increase HDL-C levels and reduce LDL-C levels. BI-5756 can also enhance the function of regulatory T cells while maintaining T cell-mediated anti-tumor activity. BI-5756 can directly inhibit the growth of tumor cells and upregulate the expression of MHC I, MHC II, and CD80 on tumor cells. BI-5756 has a protective effect in graft-versus-host disease models. BI-5756 can be used in research on tumors, graft-versus-host disease, and metabolic diseases.