MAFP (Synonyms: MAFP) |
| Katalog-Nr.GC12420 |
MAFP (Methyl Arachidonyl Fluorophosphonate) ist ein selektiver, auf das aktive Zentrum gerichteter und irreversibler Inhibitor von cPLA2 und iPLA2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 188404-10-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Methyl arachidonyl fluorophosphonate (MAFP) is a selective, active-site directed, irreversible inhibitor of cPLA2 and iPLA2.[1],[2],[3] It inhibits A23187-induced arachidonic acid release from human platelets with an IC50 value of 0.6 µM.1 The IC50 value for inhibition of iPLA2 from P388D1 cells is 0.5 µM.2 MAFP is a potent inhibitor of fatty acid amide hydrolase, exhibiting an IC50 value of 2.5 nM. MAFP also binds to the CB1 receptor in rat brain membrane preparations. The IC50 values for MAFP and arachidonyl ethanolamide in this assay are 20 and 40 nM, respectively.[4]
Reference:
[1]. Huang, Z., Liu, S., Street, I., et al. Methyl arachidonyl fluorophosphonate, a potent irreversible cPLA2 inhibitor, blocks the mobilization of arachidonic acid in human platelets and neutrophils. Mediators of Inflammation 3, 307-308 (1994).
[2]. Lio, Y.C., Reynolds, L.J., Balsinde, J., et al. Irreversible inhibition of Ca2+-independent phospholipase A2 by methyl arachidonyl fluorophosphonate. Biochimica et Biophysica Acta 1302, 55-60 (1996).
[3]. Balsinde, J., and Dennis, E.A. Distinct roles in signal transduction for each of the phospholipase A2 enzymes present in P388D1 macrophages. The Journal of Biological Chemisty 271, 6758-6765 (1996).
[4]. Deutsch, D.G., Omeir, R., Arreaza, G., et al. Methyl arachidonyl fluorophosphonate: A potent irreversible inhibitor of anandamide amidase. Biochemical Pharmacology 53, 255-260 (1997).
|
Kinase experiment: |
MAFP is dissolved and diluted in DMSO. To investigate the reversibility of iPLA 2 inhibition by MAFP, the P388D1 iPLA 2 is first concentrated approximately 10-fold using a Centricon-10 concentrator from Amicon. The concentrated iPLA 2 (20 μL) is then preincubated with either 80 μM MAFP in DMSO or DMSO alone (2 μL) for 5 min at 40°C. A 2 μL aliquot is removed and subsequently diluted 1500-fold into 3 mL of assay mixture containing 100 μM DPPC (200000 cpm per 50 μL assay mixture), 400 μM Triton X-100, 100 mM Hepes (pH 7.5), 5 mM EDTA, 1 mM DTT and 0.8 mM ATP. At the indicated time points, a 50 μL aliquot is removed and the remaining enzyme activity is quantified[1]. |
|
Cell experiment: |
Inhibition of anandamide amidase in cell culture is measured using approximately 1x106 Nl8TG2 intact neuroblastoma cells. Experimental cells are preincubated for 20 min in 1.5 mL medium, consisting of Fl2/DMEM with penicillin, streptomycin, gentamicin, 10% bovine calf serum, plus MAFP (1, 5, 10, 20 nM). Control cells contained no inhibitor. Arachidonoyl is then added and the incubation continued for I hr. The amount of [3H]anandamide in the cells is quantified by liquid scintillation counting of the silica scraped from the appropriate areas of the TLC plate identified by exposure to X-ray film[2]. |
|
References: [1]. Lio YC, et al. Irreversible inhibition of Ca(2+)-independent phospholipase A2 by methyl arachidonyl fluorophosphonate. Biochim Biophys Acta. 1996 Jul 12;1302(1):55-60. |
|
| Cas No. | 188404-10-6 | SDF | |
| Überlieferungen | MAFP | ||
| Chemical Name | (R)-methyl ((5E,8E,11E,14E)-icosa-5,8,11,14-tetraen-1-yl)phosphonofluoridate | ||
| Canonical SMILES | F[P@](OC)(CCCC/C=C/C/C=C/C/C=C/C/C=C/CCCCC)=O | ||
| Formula | C21H36FO2P | M.Wt | 370.49 |
| Löslichkeit | 3mg/mL in ethanol, or DMSO or DMF | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6991 mL | 13.4956 mL | 26.9913 mL |
| 5 mM | 0.5398 mL | 2.6991 mL | 5.3983 mL |
| 10 mM | 0.2699 mL | 1.3496 mL | 2.6991 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *