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.
HazMat Fee +
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
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].
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HazMat Fee +
