5 alpha-cholest-8(14)-en-3 beta-ol-15-one. A competitive substrate for acyl coenzyme A:cholesterol acyl transferase.
5 alpha-Cholest-8(14)-en-3 beta-ol-15-one, a potent inhibitor of cholesterol biosynthesis with hypocholesterolemic activity, has been found to serve as an efficient substrate for acyl CoA:cholesterol acyl transferase of rat hepatic and jejunal microsomes and to inhibit the esterification of cholesterol. Concentrations required to give 50% inhibition of cholesterol ester formation in liver and jejunal microsomes were approximately 10 microM and approximately 3 microM, respectively.
Miller
L R
LR
Department of Biochemistry, Rice University, Houston, TX 77251.
Needleman
D H
DH
Brabson
J S
JS
Wang
K S
KS
Schroepfer
G J
GJ
D000818:Animals; D001667:Binding, Competitive; D066298:In Vitro Techniques; D007583:Jejunum / Q000201:enzymology; D007700:Kinetics; D008297:Male; D008861:Microsomes / Q000201:enzymology; D008862:Microsomes, Liver / Q000201:enzymology; D051381:Rats; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*
D002785:Sterol O-Acyltransferase