货号:A148645 同义名: 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.
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 | USD 200+ |
规格 | 价格 | 会员价 | 库存 | 数量 | |||
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产品名称 | CB1 ↓ ↑ | CB2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Otenabant HCl |
++++
rCB1, Ki: 2.8 nM hCB1, Ki: 0.7 nM |
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AM251 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Rimonabant |
+++
hCB1, IC50: 13.6 nM |
++
hCB2, IC50: 1.64 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | FAAH ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
URB-597 |
++++
FAAH, IC50: 4.6 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
JNJ-1661010 |
+++
FAAH (human), IC50: 12 nM FAAH (rat), IC50: 10 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Biochanin A |
+
FAAH (human), IC50: 1.4 μM FAAH (mouse), IC50: 1.8 μM |
EGFR | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
PF-3845 |
++
FAAH, Ki: 230 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 188404-10-6 |
分子式 | C21H36FO2P |
分子量 | 370.481 |
别名 | Methyl Arachidonyl Fluorophosphonate |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,Store in freezer, under -20°C 液体 -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 |