An orally bioavailable inhibitor of ACAT (IC50s = 24 and 9.2 µM for ACAT1 and ACAT2

Avasimibe – 5 mg

Brand:
Cayman
CAS:
166518-60-1
Storage:
-20
UN-No:
Non-Hazardous - /

Acyl-Coenzyme A:cholesterol acyltransferases (ACAT1 and ACAT2) 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.{20948} Avasimibe is an orally bioavailable inhibitor of ACAT (IC50s = 24 and 9.2 µM for ACAT1 and ACAT2, respectively).{21762} It reduces foam cell formation in human macrophages in vitro, enhancing free cholesterol efflux and inhibiting the uptake of modified LDL and dose-dependently reduces plasma total triglyceride and VLDL cholesterol levels in cholesterol-fed animal models.{29393,29394} Avasimibe inhibition of ACAT has been used to decrease amyloid β generation in models of Alzheimer’s disease.{29395}  

 

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Description

An orally bioavailable inhibitor of ACAT (IC50s = 24 and 9.2 µM for ACAT1 and ACAT2, respectively) that reduces plasma total triglyceride and VLDL cholesterol levels in cholesterol-fed animal models; also used to decrease amyloid β generation in models of Alzheimer’s disease

Formal name: 2,6-bis(1-methylethyl)phenyl ester N-[2-[2,4,6-tris(1-methylethyl)phenyl]acetyl]-sulfamic acid

Synonyms:  Cl-1011|PD-148515

Molecular weight: 501.7

CAS: 166518-60-1

Purity: ≥98%

Formulation: A crystalline solid

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|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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