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CAS No.: 188404-10-6

MAFP Catalog No. CSN25339

Synonyms: Methyl Arachidonyl Fluorophosphonate

MAFP is a potent, irreversible inhibitor of fatty acid amide hydrolase (FAAH, anandamide amidase), the enzyme responsible for anandamide hydrolysis (IC50 = 2.5 nM). MAFP also binds irreversibly to CB1 receptors with IC50 of 20 nM.

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技术信息

生物活性

描述Phthiocerol dimycocerosates and phenolic glycolipids (PGL) are considered as major virulence elements of Mycobacterium tuberculosis, in particular because of their involvement in cell wall impermeability and drug resistance. The biosynthesis of these waxy lipids involves multiple enzymes, including thioesterase A (TesA). Methyl arachidonyl fluorophosphonate (MAFP) inhibits Mycobacterium tuberculosis thioesterase TesA and globally affects vancomycin susceptibility. MAFP increased by more than 10-fold the susceptibility of M. bovis BCG to vancomycin. The MIC of MAFP dropped from ≥ 10 to 1 μg/mL in the presence of vancomycin (25 μg/mL), and the MIC of vancomycin dropped from ≥ 500 to25 μg/mL in the presence of MAFP (1 μg/mL), showing that this combination can inhibit M. bovis BCG growth in synergy (FICI < 0.15). MAFP inhibited TesA TE activity in a concentration-dependent manner. With MAFP, a maximal 52% inhibition was observed in all tested experimental conditions, for example the competitive assay or by preincubating TesA with MAFP for 5 or 20 min before starting the reaction with palmitoyl-CoA^[1].
作用机制MAFP docks into one of the two binding sites of the dimer. Most of the MAFP poses occupy the second binding site with the fluorophosphonate matching the crystal ligand phosphate^[1].
参考文献

[1] Yang D, Vandenbussche G, Vertommen D, et al. Methyl arachidonyl fluorophosphonate inhibits Mycobacterium tuberculosis thioesterase TesA and globally affects vancomycin susceptibility. FEBS Lett. 2020;594(1):79-93

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6992 mL
- 13.4960 mL
- 26.9919 mL
- 5 mM
- 0.5398 mL
- 2.6992 mL
- 5.3984 mL
- 10 mM
- 0.2699 mL
- 1.3496 mL
- 2.6992 mL

技术信息

CAS号	188404-10-6	储存条件	粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C21H36FO2P	运输	蓝冰
分子量	370.48	别名	Methyl Arachidonyl Fluorophosphonate

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