Melinamide
Based on 1 Customer Validation
Melinamide, an amide derivative of an unsaturated long-chain fatty acid, is an inhibitor of cholesterol absorption with an IC50 of 20.9 μM.
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- Reinheit: 99.9%
- CAS. Nr.: 14417-88-0
- Formel: C26H41NO
- Molecular Weight:383.61
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Speicherung:Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Biologische Aktivität
IC50: 20.9 μM (cholesterol)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | CC50 |
95.8 μM
Compound: 2b
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Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33479624] |
| THP-1 | IC50 |
5.2 μM
Compound: 2b
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Inhibition of LPS-induced TNFalpha production in human THP-1 cells incubated for 2 hrs followed by LPS stimulation and measured after 12 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in human THP-1 cells incubated for 2 hrs followed by LPS stimulation and measured after 12 hrs by ELISA
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[PMID: 33479624] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 14417-88-0
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Appearance Oil
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Molecular Weight 383.61
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Formel C26H41NO
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Color Colorless to light yellow
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SMILES
CCCCC/C=C\C/C=C\CCCCCCCC(NC(C1=CC=CC=C1)C)=O
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Synonyms
AC 223; DL-N-(α-Methylbenzyl)linoleamide
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (260.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (268 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6068 mL | 13.0341 mL | 26.0681 mL | 65.1704 mL |
| 5 mM | 0.5214 mL | 2.6068 mL | 5.2136 mL | 13.0341 mL | |
| 10 mM | 0.2607 mL | 1.3034 mL | 2.6068 mL | 6.5170 mL | |
| 15 mM | 0.1738 mL | 0.8689 mL | 1.7379 mL | 4.3447 mL | |
| 20 mM | 0.1303 mL | 0.6517 mL | 1.3034 mL | 3.2585 mL | |
| 25 mM | 0.1043 mL | 0.5214 mL | 1.0427 mL | 2.6068 mL | |
| 30 mM | 0.0869 mL | 0.4345 mL | 0.8689 mL | 2.1723 mL | |
| 40 mM | 0.0652 mL | 0.3259 mL | 0.6517 mL | 1.6293 mL | |
| 50 mM | 0.0521 mL | 0.2607 mL | 0.5214 mL | 1.3034 mL | |
| 60 mM | 0.0434 mL | 0.2172 mL | 0.4345 mL | 1.0862 mL | |
| 80 mM | 0.0326 mL | 0.1629 mL | 0.3259 mL | 0.8146 mL | |
| 100 mM | 0.0261 mL | 0.1303 mL | 0.2607 mL | 0.6517 mL |
Melinamide Related Classifications
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