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CETP inhibitors

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By Targets:	CETP (19) Apolipoprotein (3) Cannabinoid Receptor (1) Drug Intermediate (1) HMG-CoA Reductase (HMGCR) (1) LDLR (3) LPL Receptor (3) MHC (1) PCSK9 (2) PPAR (1) Reference Standards (3)
By Research Areas:	Cancer (3) Cardiovascular Disease (15) Endocrinology (1) Inflammation/Immunology (1) Metabolic Disease (7)

Inhibitors & Agonists

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Targets Recommended: CETP Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13327

Evacetrapib 3 Publications Verification LY2484595	CETP	Cardiovascular Disease
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-18778

Obicetrapib TA-8995; DEZ-001; AMG-899	CETP Apolipoprotein LPL Receptor LDLR	Cardiovascular Disease
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) .

HY-12090

Anacetrapib 3 Publications Verification MK-0859	PCSK9	Cardiovascular Disease
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-14950

Dalcetrapib 2 Publications Verification JTT-705; RO4607381	CETP	Cardiovascular Disease Cancer
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 .

HY-12089

Torcetrapib CP-529414	CETP	Endocrinology
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-116078

CKD-519	CETP	Cardiovascular Disease
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-W414588

Colestolone	HMG-CoA Reductase (HMGCR) CETP	Metabolic Disease
Colestolone is a 15-ketosterol compound and an orally active inhibitor of HMG-CoA reductase. Colestolone can inhibit the activity of cholesteryl ester transfer protein (CETP) in vitro (IC₅₀= 660 μM). Colestolone is a cholesterol-lowering agent, and can be used in the research of endocrine and metabolic diseases such as hyperlipidemia .

HY-W015752

5-Methoxyresorcinol	Drug Intermediate	Others
5-Methoxyresorcinol is a model molecule of the A ring of flavonoids, specifically simulating the chemical behavior of the resorcinol-type A ring found in catechins. 5-Methoxyresorcinol exhibits extremely low reactivity of tocopherol. 5-Methoxyresorcinol hardly inhibits cholesteryl ester transfer protein (CETP) .

HY-171883

BI-5756	Cannabinoid Receptor CETP MHC	Metabolic Disease Inflammation/Immunology Cancer
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 .

HY-107997

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

HY-123039

CP-532623	CETP	Metabolic Disease
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 .

HY-19614

BMS-795311	CETP	Cardiovascular Disease
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-105316

CP-800569	CETP	Metabolic Disease
CP-800569 is an orally active cholesteryl ester transfer protein (CETP) inhibitor. CP-800569 can decrease low-density lipoprotein and postprandial triglyceride and increase high-density lipoprotein. CP-800569 can be used for the research of metabolic disease .

HY-107054

ESP-31015 ETC-1001	PPAR	Cardiovascular Disease
ESP-31015 (ETC-1001) is an orally active and non-fibrate based PPARα agonists. ESP-31015 demonstrates significant lipid-regulating effects in the obese Zucker rat model. ESP-31015 can be used in cardiovascular disease research .

HY-142643

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

HY-128338

CETP-IN-3	CETP	Cardiovascular Disease
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-13327R

Evacetrapib (Standard) LY2484595 (Standard)	CETP Reference Standards	Cardiovascular Disease
Evacetrapib (Standard) is the analytical standard of Evacetrapib. This product is intended for research and analytical applications. 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-14950R

Dalcetrapib (Standard) JTT-705 (Standard); RO4607381 (Standard)	CETP Reference Standards	Cardiovascular Disease Cancer
Dalcetrapib (Standard) is the analytical standard of Dalcetrapib. This product is intended for research and analytical applications. 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 .

HY-12090R

Anacetrapib (Standard) MK-0859 (Standard)	PCSK9 Reference Standards	Cardiovascular Disease
Anacetrapib (Standard) is the analytical standard of Anacetrapib. This product is intended for research and analytical applications. 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-132303

MK-8262	CETP	Cardiovascular Disease Metabolic Disease
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-18778B

Obicetrapib potassium TA-8995 potassium; DEZ-001 potassium; AMG-899 potassium	Apolipoprotein CETP LPL Receptor LDLR	Metabolic Disease
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) .

HY-18778A

Obicetrapib sodium TA-8995 sodium; DEZ-001 sodium; AMG-899 sodium	Apolipoprotein CETP LPL Receptor LDLR	Cardiovascular Disease
Obicetrapib (TA-8995; DEZ-001) sodium is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib sodium potently reduces atherogenic lipoproteins (such as LDL-C, ApoB, Lp (a)) and increases HDL-C. Obicetrapib sodium can be used for the research of dyslipidemia and atherosclerotic cardiovascular disease (ASCVD) .

HY-182320

DRL-17822	CETP	Cardiovascular Disease
DRL-17822 is a selective cholesteryl ester transfer protein (CETP) inhibitor. DRL-17822 increases high-density lipoprotein levels. The exposure of DRL-17822 nanocrystal formulation increases significantly after a high-fat breakfast. The exposure of DRL-17822 in the fasted state is higher than that of its nanocrystal formulation. DRL-17822 can be used in the research of type II hyperlipidemia and atherosclerotic cardiovascular disease .

5-Methoxyresorcinol	Classification of Application Fields Other Diseases Phenols Polyphenols Endogenous metabolite Disease Research Fields Source Classification	Drug Intermediate
5-Methoxyresorcinol is a model molecule of the A ring of flavonoids, specifically simulating the chemical behavior of the resorcinol-type A ring found in catechins. 5-Methoxyresorcinol exhibits extremely low reactivity of tocopherol. 5-Methoxyresorcinol hardly inhibits cholesteryl ester transfer protein (CETP) .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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CETP inhibitors

Inhibitors & Agonists

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