Melinamide
(Synonyms: 甲亚油酰胺; AC 223; DL-N-(α-Methylbenzyl)linoleamide) 目录号 : GC19243
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。
Cas No.:14417-88-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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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]. |
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References: [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. |
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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].
References:
[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.
| Cas No. | 14417-88-0 | SDF | |
| 别名 | 甲亚油酰胺; AC 223; DL-N-(α-Methylbenzyl)linoleamide | ||
| Canonical SMILES | CCCCC/C=C\C/C=C\CCCCCCCC(NC(C1=CC=CC=C1)C)=O | ||
| 分子式 | C26H41NO | 分子量 | 383.61 |
| 溶解度 | DMSO : 200 mg/mL (521.36 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6068 mL | 13.0341 mL | 26.0681 mL |
| 5 mM | 0.5214 mL | 2.6068 mL | 5.2136 mL |
| 10 mM | 0.2607 mL | 1.3034 mL | 2.6068 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。