F1394 is an orally available, potent and selective Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor that reduces plaque foam cell formation without inflammatory or toxic effects.
Orally available, potent and selective Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor
Acyl-CoA:cholesterol acyltransferase (ACAT) mediates cellular cholesterol esterification. In atherosclerotic plaque macrophages, ACAT promotes cholesteryl ester accumulation, resulting in foam cell formation and atherosclerosis progression. Its complete inactivation in mice, however, showed toxic effects because of an excess of free cholesterol
British journal of pharmacology, 133(7), 1005-1012 (2001-08-07)
The acyl-CoA:cholesterol acyltransferase (ACAT) enzyme is thought to be responsible for foam cell formation and the subsequent progression of atherosclerosis. The apolipoprotein E and low density lipoprotein receptor double knockout (apoE/LDLr-DKO) mouse is an animal model that develops severe hyperlipidaemia
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