cholesterol acyltransferase

Eflucimibe (L0081) is an acyl coenzyme A: cholesterol acyltransferase inhibitor for the treatment of cardiovascular disease and endocrine and metabolic disorders, and can be used to study atherosclerosis and hyperlipidemia.

Lecimibide (DuP 128) is a potent and selective inhibitor of acyl coenzyme A:cholesterol acyltransferase (ACAT), useful for studying high-lipid-related diseases.

VULM 1457 is a potent ACAT inhibitor. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells.

ACAT-IN-10 is an acyl-Coenzyme A: cholesterol acyltransferase (ACAT) inhibitor that exhibits weak inhibitory activity on NF-κB-mediated transcription.

Acyl-coenzyme A: cholesterol acyltransferase-1 and -2 (ACAT-1 and ACAT-2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis. CAY10485 inhibits human ACAT-1 and ACAT-2 with an IC50 values of 95 and 81 μM, respectively. It also inhibits copper-mediated oxidation of low density lipoproteins by 91% at a concentration of 2 μM.

AcylCoA:cholesterol acyltransferase (ACAT) is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleyl analide (OA) is a weak inhibitor of acylCoA:cholesterol acyltransferase (ACAT) with an IC50 of 26 μM. OA and the related glyceride dioleoyl phenylamino propane 1,2-diol have been linked to a syndrome of eosinophilia, excessive T-cell activation, and elevated interleukin-4 (IL-4), soluble IL-2R, and IL-5. The clinical consequences are an acute pulmonary inflammatory reaction followed by chronic neuropathy, myalgia, and autoimmune connective tissue disease, generally referred to as toxic oil syndrome (TOS). Aniline-denatured cooking oil is a source of OA associated with TOS.

Beauveriolide I is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.78 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide I also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 6 μM).2 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

Pomonic acid, a triterpenoid compound, effectively inhibits cholesterol ester accumulation and suppresses acyl coenzyme A:cholesterol acyltransferase (ACAT) activity [1].

Beauveriolide III is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.41 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide III also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 5.5 μM).2Beauveriolide III (25 and 50 mg/kg) reduces the size of aortic atherosclerotic lesions inLdlr-/-andApoE-/-mouse models of atherosclerosis. 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

Yakuchinone B is an acyl-CoA:cholesterol O-acyltransferase (ACAT) inhibitor with cholesterol-lowering activity, identified in the seeds of the Zingiberaceae family. It inhibits rat liver ACAT with an IC50 value of 20.6 μM. Yakuchinone B is a potential candidate for research into hypercholesterolemia and atherosclerosis.

ACAT-IN-5 (example 19) is an inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT) that effectively suppresses NF-κB-mediated transcription.

ACAT-IN-9, acts as an inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT). By doing so, it effectively suppresses NF-κB mediated transcription.

Oleic acid-2,6-diisopropylanilide is an inhibitor of acylCoA:cholesterol acyltransferase (ACAT), an intracellular cholesteryl ester synthase involved in dietary cholesterol absorption, with an IC50 of 7 nM. When administered at 0.05% to rabbits or rats on a high fat, high cholesterol diet, it reduces low-density lipoproteins and increases high-density lipoprotein levels.

SMP-797 HCl, an ACAT (acyl-CoA-cholesterol acyltransferase) inhibitor, is used potentially for the treatment of Hyperlipidemia.

Enniatin A, a Fusarium mycotoxin, inhibits acyl-CoA: cholesterol acyltransferase (ACAT) with an IC50 of 22 μM in rat liver microsome enzyme assays.

CP-113818 is a potent inhibitor of cholesterol acyltransferase (ACAT) and can be used to study Alzheimer's disease.

ACAT-IN-2 is a potent inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT). This compound effectively blocks NF-κB mediated transcription.

ACAT-IN-3, a potent inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT), effectively suppresses NF-κB dependent transcription.

Acyl-Coenzyme A: cholesterol acyltransferase-1 and -2 (ACAT-1 and ACAT-2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis. CAY10486 inhibits human ACAT-1 and ACAT-2 equally with an IC50 value of approximately 60 μM. It also inhibits copper-mediated oxidation of low density lipoproteins by about 28% at a concentration of 3 μM.

Acaterin, an inhibitor of acyl-CoA: cholesterol acyltransferase (ACAT), inhibits synthesis of cholesteryl ester in macrophage J774.

F-1394 is an acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. F-1394 both prevents the formation of atherosclerosis and accelerates its regression without affecting the serum TC level, indicating that F-1394 acts directly on the arterial wall. F-1394 significantly reduced neointimal thickening and the extent of macrophages in lesions without affecting serum cholesterol levels. In vitro, F-1394 attenuated foam cell formation in mouse peritoneal macrophages.

ACAT-IN-10 dihydrochloride is a compound that serves as an inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT).ACAT-IN-10 dihydrochloride effectively hampers NF-κB mediated transcription, albeit to a lesser extent.

ACAT-IN-7 is a compound that acts as an inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT) enzyme. It effectively suppresses the transcription process mediated by NF-κB.

Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 |1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of acyl-CoA: Cholesterol acyltransferase produced by Penicillium griseofulvum F1959. J. Antibiot. (Tokyo) 55(11), 1004-1008 (2002).|2. Lee, S.W., Rho, M.C., Choi, J.H., et al. Inhibition of diacylglycerol acyltransferase by phenylpyropenes produced by Penicillium griseofulvum F1959. J. Microbiol. Biotechnol. 18(11), 1785-1788 (2008).|3. Horikoshi, R., Goto, K., Mitomi, M., et al. Identification of pyripyropene A as a promising insecticidal compound in a microbial metabolite screening. J. Antibiot. (Tokyo) 70(3), 272-276 (2017).