2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Acyltransferase
  5. ACAT1 Isoform

ACAT1

ACAT1, also termed sterol O-acyltransferase 1 (SOAT1), is an endoplasmic reticulum-associated enzyme that catalyzes the conversion of free cholesterol and long-chain fatty acyl-CoA into cholesteryl esters, thereby maintaining intracellular cholesterol homeostasis and promoting lipid droplet formation[1][6]. Mechanistically, ACAT1-mediated cholesterol esterification limits excess free cholesterol accumulation and regulates cholesterol storage, linking membrane cholesterol balance to cellular metabolic adaptation[1][7]. In macrophages, increased cholesterol influx activates ACAT1 and drives cholesteryl ester deposition, a process closely associated with foam-cell formation and early atherosclerotic lesion development[8][2]. Experimental inhibition of ACAT activity enhances the pool of free cholesterol available for efflux and alters macrophage cholesterol metabolism, making ACAT1 a widely studied target in atherosclerosis models[8][2]. Beyond cardiovascular disease, dysregulated ACAT1-dependent cholesterol esterification has been reported in cancer and neurodegenerative disorders, where elevated cholesteryl ester accumulation is linked to altered cellular cholesterol handling[6][3][4]. Compared with the related isoform ACAT2/SOAT2, which is enriched in intestine and liver and participates in lipoprotein-associated cholesteryl ester production, ACAT1 is broadly expressed in peripheral tissues and is the dominant isoform involved in macrophage cholesterol storage and foam-cell biology[9][5]. For experimental applications, inhibitors including avasimibe and the ACAT1-selective compound K-604 have been used to investigate cholesterol esterification, plaque remodeling, and disease-associated lipid metabolic pathways[2][10].

ACAT1 Related Products (7):

Cat. No. Product Name Effect Purity
  • HY-13215
    Avasimibe
    		Inhibitor 99.85%
    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
    		Inhibitor 99.42%
    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-100399A
    Nevanimibe hydrochloride
    		Inhibitor 99.49%
    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
    		Inhibitor 99.98%
    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 Ki 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-100399
    Nevanimibe
    		Inhibitor 98.99%
    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-N18066
    Esculeogenin A
    		Inhibitor
    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-100401A
    Pactimibe sulfate
    		Inhibitor 98.0%
    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.
Cat. No. Product Name / Synonyms Application Reactivity