MAFP

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Chemical Structure| 188404-10-6 同义名 : Methyl Arachidonyl Fluorophosphonate
CAS号 : 188404-10-6
货号 : A148645
分子式 : C21H36FO2P
纯度 : 95%
分子量 : 370.481
MDL号 : MFCD03095722
存储条件：

Pure form Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(283.41 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.50mL

2.70mL

1.35mL

26.99mL

5.40mL

2.70mL
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