Melinamide

Melinamide 是一种不饱和长链脂肪酸的酰胺衍生物，是一种胆固醇吸收抑制剂，IC50 为 20.9 μM。

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5mg

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货号: ajci22728
CAS: 14417-88-0
别名: 甲亚油酰胺; AC 223; DL-N-(α-Methylbenzyl)linoleamide
分子式: C26H41NO
分子量: 383.61
纯度: >98%
溶解度: Soluble in DMSO
储存: Store at -20°C
库存: 现货

Background

Melinamide, an amide derivative of an unsaturated long-chain fatty acid, is an inhibitor of cholesterol absorption with an IC50 of 20.9 uM.

DL-Melinamide inhibits acyl CoA:cholesterol acyltransferase activity (ACAT) in the mucosal microsomes, with 50% inhibition occurring at approximately 0.5 uM. 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].

参考文献:
[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):357-65.
[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.

Protocol

Animal experiment:

Rats: 10 diabetic rats are divided into two groups: a cholesterol-fed diabetic group and a melinamide-treated cholesterol-fed diabetic group. Five control rats are injected with citrate buffer only. The rats are fed each diet for 3 weeks after injection. The chol-fed DM group receives a diet (20 g/day) containing 1% cholesterol, 0.5% cholic acid and 5% lard. The melinamide-treated group receives the same diet but supplemented with 0.1% melinamide. Control rats are fed a standard chow (20 g/day). Following a 24-h fast the animals are killed. Blood is collected by aortic puncture and samples of small intestine are retained[3].

参考文献:

[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):357-65.
[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.