1. Metabolic Enzyme/Protease
  2. Phospholipase
  3. MAFP

MAFP  (Synonyms: Methyl Arachidonyl Fluorophosphonate)

Art. -Nr.: HY-103334 Reinheit: 98.6%
Handling Instructions Technical Support

MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.

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MAFP

MAFP Chemische Struktur

CAS. Nr. : 188404-10-6

Größe Preis Verfügbarkeit Menge
Solvent
1 mg (26.99 mM * 100 μL in Methyl acetate) Auf Lager
Solvent
5 mg (26.99 mM * 500 μL in Methyl acetate) Auf Lager
Solvent
10 mg (26.99 mM * 1 mL in Methyl acetate) Auf Lager
Solvent
25 mg (26.99 mM * 2.5 mL in Methyl acetate) Auf Lager
Solvent
50 mg (26.99 mM * 5 mL in Methyl acetate) Auf Lager
Solvent
100 mg (26.99 mM * 10 mL in Methyl acetate) Auf Lager

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Based on 5 publication(s) in Google Scholar

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Beschreibung

MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.

IC50 & Target

cPLA2, iPLA2[1], Anandamide amidase[2]

In Vitro

MAFP inhibits iPLA2, in a concentration-dependent manner with an IC50 of 0.5 μM after a 5 min preincubation at 40°C in P388D1 cells. cPLA, is a phospholipid hydrolase using the hydroxyl of serine-228 residue as its catalytic nucleophile[1]. MAFP is also an inhibitor of anandamide amidase and as a ligand for the CB1 cannabinoid receptor. MAFP demonstrates selectivity towards anandamide amidase for which it is approximately 3000 and 30000-fold more potent than it is towards chymotrypsin and trypsin, respectively. MAFP displaces [3H]CP-55940 binding to the CB1 cannabinoid receptor with an IC50 of 20 nM vs 40 nM for anandamide[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molekulargewicht

370.48

Formel

C21H36FO2P

CAS. Nr.
Appearance

Liquid (Density: 0.960±0.06 g/cm3)

Color

Colorless to light yellow

SMILES

CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCCP(OC)(F)=O

Versand

Shipping with dry ice.

Speicherung

-80°C, protect from light

Reinheit & Dokumentation

Purity: 98.6%

Verweise
Kinase-Assay
[1]

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].

MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.

Zellassay
[2]

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].

MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.

Verweise
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  • Molaritätsrechner

  • Verdünnungsrechner

Die Formel zur Berechnung von Molaritäten

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)

Diese Gleichung wird häufig abgekürzt als: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MAFP
Art. -Nr.:
HY-103334
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