For research use only. Not for therapeutic Use.
Melinamide, an amide derivative of an unsaturated long-chain fatty acid, is an inhibitor of cholesterol absorption with an IC50 of 20.9 μM.
DL-Melinamide inhibits acyl CoA:cholesterol acyltransferase activity (ACAT) in the mucosal microsomes, with 50% inhibition occurring at approximately 0.5 μM. Kinetic studies indicate that DL-Melinamide is an uncompetitive inhibitor of acyl CoA:cholesterol acyltransferase. D-Melinamide is found to be a more effective inhibitor than L-Melinamide[2].
Melinamide is a new hypocholesterolaemic drug. Melinamide causes a substantial decrease of the enhanced intestinal ACAT activity in diabetic rats, but does not affect intestinal cholesterol esterase activity. Furthermore, marked improvement of hypercholesterolaemia in cholesterol-fed diabetic rats occurrs concomitantly with the drug treatment[3].
| Catalog Number | M063088 |
| CAS Number | 14417-88-0 |
| Synonyms | (9Z,12Z)-N-(1-phenylethyl)octadeca-9,12-dienamide |
| Molecular Formula | C26H41NO |
| Purity | ≥95% |
| InChI | InChI=1S/C26H41NO/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-16-20-23-26(28)27-24(2)25-21-18-17-19-22-25/h7-8,10-11,17-19,21-22,24H,3-6,9,12-16,20,23H2,1-2H3,(H,27,28)/b8-7-,11-10- |
| InChIKey | RWIUTHWKQHRQNP-NQLNTKRDSA-N |
| SMILES | CCCCCC=CCC=CCCCCCCCC(=O)NC(C)C1=CC=CC=C1 |
| Reference | [1]. Kusunoki J, et al. Effect of F-1394, a potent and selective inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), on esterification of cholesterol and basolateral secretion of cholesteryl ester in Caco-2 cells Nihon Yakurigaku Zasshi. 1997 Dec;110(6): [2]. Natori K, et al. Mechanism of the inhibition of cholesterol absorption by DL-melinamide: inhibition of cholesterol esterification. Jpn J Pharmacol. 1986 Dec;42(4):517-23. [3]. Matsubara K, et al. Cholesterol-lowering effect of N-(alpha-methylbenzyl)linoleamide (melinamide) in cholesterol-fed diabetic rats. Atherosclerosis. 1988 Aug;72(2-3):199-204. |
