A potent inhibitor of ACAT2 (IC50 = 70 nM) with high selectivity over the ACAT1 isozyme (IC50 > 80 μM); 10-50 mg/kg per day for 12 weeks lowers plasma and hepatic cholesterol

Pyripyropene A – 1 mg

Brand:
Cayman
CAS:
147444-03-9
Storage:
-20
UN-No:
Non-Hazardous - /

Acyl-CoA: cholesterol acyltransferase (ACAT) is a key enzyme for cholesteryl ester accumulation in atherogenesis, lipoprotein formation in liver, and cholesterol absorption from intestines, all of which are events that contribute to the atherosclerotic process.{13122,14056} Two ACAT isozymes have been identified and are expressed in distinct tissues. ACAT1 is ubiquitously expressed at a high level in sebaceous glands, steroidogenic tissues, and macrophages, whereas ACAT2 is expressed predominantly in the liver and intestine.{11763} Pyripyropene A, naturally produced by A. fumigates, is a potent inhibitor of ACAT2 with an IC50 value of 70 nM in an in vitro activity assay.{21763,21761,21762} It demonstrates high selectivity for the ACAT2 isozyme, inhibiting ACAT1 in a similar assay with an IC50 value of > 80 μM.{21762} A dose of 10 to 100 mg/kg PPPA inhibits cholesterol absorption in mouse intestine by 30.5-55%.{21762} Oral administration to apolipoprotein E-knockout mice at 10-50 mg/kg per day for 12 weeks can lower the levels of plasma cholesterol and hepatic cholesterol, very-low-density lipoprotein, and LDL content, resulting in protection from atherosclerosis development.{21762}  

 

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Description

A potent inhibitor of ACAT2 (IC50 = 70 nM) with high selectivity over the ACAT1 isozyme (IC50 > 80 μM); 10-50 mg/kg per day for 12 weeks lowers plasma and hepatic cholesterol, VLDL, and LDL content in apolipoprotein E-knockout mice

Formal name: 3,6-bis(acetyloxy)-4-[(acetyloxy)methyl]-1,3S,4R,4aR,5,6S,6aS,12R,12aS,12bS-decahydro-12-hydroxy-4,6a,12b-trimethyl-9-(3-pyridinyl)-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-11-one

Synonyms:  FO-1289A|PPPA

Molecular weight: 583.6

CAS: 147444-03-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Natural Products|Microbial Metabolites||Product Type|Biochemicals|Small Molecule Inhibitors|Acyltransferases||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Cardiovascular System|Lipids & Lipoproteins|Cholesterol Metabolism||Research Area|Cardiovascular System|Lipids & Lipoproteins|Lipoproteins||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Dyslipidemias

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