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Acat 1 Inhibitors

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By Targets:	Acyltransferase (14) Apoptosis (3) Drug Derivative (1) Fatty Acid Synthase (FASN) (1) Fungal (1) Keap1-Nrf2 (1) NF-κB (1) Parasite (1) PPAR (1) Reference Standards (4)
By Research Areas:	Cancer (5) Cardiovascular Disease (7) Infection (1) Inflammation/Immunology (1) Metabolic Disease (3)

Inhibitors & Agonists

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Targets Recommended: Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13215

Avasimibe Maximum Cited Publications 17 Publications Verification CI-1011; PD-148515	Acyltransferase	Cancer
Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC₅₀s of 24 and 9.2 µM for *ACAT1* and *ACAT2*, respectively . Avasimibe can be used for the research of prostate cancer .

HY-100400A

K-604 dihydrochloride 5+ Cited Publications	Acyltransferase	Cardiovascular Disease
K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC₅₀ of 0.45±0.06 μM.

HY-111880

γ-Sanshool	Acyltransferase	Cardiovascular Disease
γ-Sanshool can be isolated from Zanthoxylum piperitum. γ-Sanshool inhibits human *ACAT-1* and *ACAT-2* activities with IC₅₀s of 12.0 and 82.6 μM .

HY-100399

Nevanimibe 3 Publications Verification PD-132301; ATR-101	Acyltransferase Apoptosis	Cancer
Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC₅₀ of 9 nM. Nevanimibe inhibits ACAT2 with an EC₅₀ of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer .

HY-100399A

Nevanimibe hydrochloride 3 Publications Verification PD-132301 hydrochloride; ATR101 hydrochloride	Acyltransferase Apoptosis	Cancer
Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC₅₀ of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC₅₀ of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer .

HY-100401

Pactimibe CS-505 free base	Acyltransferase	Cardiovascular Disease
Pactimibe (CS-505 free base) is a dual *ACAT1/2* inhibitor with IC₅₀s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits *ACAT* with IC₅₀s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively . Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a K_i value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC₅₀ of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .

HY-100401A

Pactimibe sulfate CS-505	Acyltransferase	Cardiovascular Disease
Pactimibe sulfate (CS-505) is a dual *ACAT1/2* inhibitor with IC₅₀s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits *ACAT* with IC₅₀s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively . Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a K_i value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC₅₀ of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .

HY-120082

FR-182980	Acyltransferase	Metabolic Disease
FR-182980 is an orally active *ACAT1* inhibitor (IC₅₀: 30 nM). FR-182980 has hypocholesterolemic activity and can be used for research of atherosclerosis .

HY-100400AR

K-604 dihydrochloride (Standard)	Reference Standards Acyltransferase	Cardiovascular Disease
K-604 (dihydrochloride) (Standard) is the analytical standard of K-604 (dihydrochloride). This product is intended for research and analytical applications. K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45±0.06 μM.

HY-13215R

Avasimibe (Standard) CI-1011 (Standard); PD-148515 (Standard)	Acyltransferase Reference Standards	Cancer
Avasimibe (Standard) is the analytical standard of Avasimibe. This product is intended for research and analytical applications. Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively . Avasimibe can be used for the research of prostate cancer .

HY-100399AR

Nevanimibe hydrochloride (Standard) PD-132301 hydrochloride (Standard); ATR101 hydrochloride (Standard)	Reference Standards Acyltransferase Apoptosis	Cancer
Nevanimibe hydrochloride (Standard) is the analytical standard of Nevanimibe hydrochloride. This product is intended for research and analytical applications. Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer .

HY-N14968

Enniatin F	Parasite Fungal	Infection
Enniatin F has insecticidal and antifungal activity. Enniatin F also can inhibit acyl-CoA, cholesterol acyltransferase (ACAT) .

HY-118486

LDL-IN-1	Acyltransferase	Metabolic Disease
LDL-IN-1 (Compound 1) is an antioxidant, and is active against copper mediated LDL oxidation (IC₅₀ = 52 μM). LDL-IN-1 is also an Acyl-CoA:cholesterol acyltransferase-1 and -2 (ACAT-1/2) inhibitor, with IC₅₀s of 60 μM. LDL-IN-1 can be used for anti-atherosclerotic research .

HY-N18066

Esculeogenin A	Drug Derivative Acyltransferase NF-κB PPAR Fatty Acid Synthase (FASN) Keap1-Nrf2	Cardiovascular Disease Metabolic Disease Inflammation/Immunology
Esculeogenin A is the sapogenol of tomato saponin Esculeoside A (HY-N18067). Esculeogenin A is an orally active hepatoprotective, hypolipidemic, and antioxidant agent. Esculeogenin A regulates molecular targets like PPARα, SREBP1, Nrf2, NF-κB, *ACAT1/ACAT2* to promote hepatic fatty acid oxidation, suppress de novo lipogenesis, enhance antioxidant defense, and inhibit inflammation. Esculeogenin A improves liver function, alleviates hyperlipidemia, and inhibits hepatic steatosis and foam cell formation, preventing nonalcoholic fatty liver disease in high-fat-diet-fed rats and reducing atherosclerotic lesions in apoE-deficient mice. Esculeogenin A can be used for the research of nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia .

HY-100401AR

Pactimibe sulfate (Standard) CS-505 (Standard)	Acyltransferase Reference Standards	Cardiovascular Disease
Pactimibe (sulfate) (Standard) is the analytical standard of Pactimibe (sulfate) (HY-100401A). This product is intended for research and analytical applications. Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively . Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .

γ-Sanshool	Zanthoxylum bungeanum Maxim. Structural Classification Alkaloids Other Alkaloids Rutaceae Plants Source Classification	Acyltransferase
γ-Sanshool can be isolated from Zanthoxylum piperitum. γ-Sanshool inhibits human *ACAT-1* and *ACAT-2* activities with IC₅₀s of 12.0 and 82.6 μM .

Enniatin F	Natural Products Microorganisms Source Classification	Parasite Fungal
Enniatin F has insecticidal and antifungal activity. Enniatin F also can inhibit acyl-CoA, cholesterol acyltransferase (ACAT) .

Esculeogenin A	Structural Classification Solanum lycopersicum L. Solanaceae Plants Steroids Source Classification	Drug Derivative Acyltransferase NF-κB PPAR Fatty Acid Synthase (FASN) Keap1-Nrf2
Esculeogenin A is the sapogenol of tomato saponin Esculeoside A (HY-N18067). Esculeogenin A is an orally active hepatoprotective, hypolipidemic, and antioxidant agent. Esculeogenin A regulates molecular targets like PPARα, SREBP1, Nrf2, NF-κB, *ACAT1/ACAT2* to promote hepatic fatty acid oxidation, suppress de novo lipogenesis, enhance antioxidant defense, and inhibit inflammation. Esculeogenin A improves liver function, alleviates hyperlipidemia, and inhibits hepatic steatosis and foam cell formation, preventing nonalcoholic fatty liver disease in high-fat-diet-fed rats and reducing atherosclerotic lesions in apoE-deficient mice. Esculeogenin A can be used for the research of nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia .

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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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Acat 1 Inhibitors

Inhibitors & Agonists

NaturalProducts

Natural
Products