| Bioactivity | Melinamide, an amide derivative of an unsaturated long-chain fatty acid, is an inhibitor of cholesterol absorption with an IC50 of 20.9 μM. | ||||||||||||
| Target | IC50: 20.9 μM (cholesterol) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | Melinamide | ||||||||||||
| CAS | 14417-88-0 | ||||||||||||
| Formula | C26H41NO | ||||||||||||
| Molar Mass | 383.61 | ||||||||||||
| Appearance | Oil | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |