A cPLA2 inhibitor
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AX 048

Item No. 13823

Technical Information
Formal Name
4-[(1,2-dioxohexadecyl)amino]-butanoic acid, ethyl ester
CAS Number
873079-69-7
Molecular Formula
C22H41NO4
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 10 mg/mlDMSO: 2 mg/mlEthanol: 5 mg/ml
λmax
242 nm
SMILES
O=C(C(NCCCC(OCC)=O)=O)CCCCCCCCCCCCCC
InChi Code
InChI=1S/C22H41NO4/c1-3-5-6-7-8-9-10-11-12-13-14-15-17-20(24)22(26)23-19-16-18-21(25)27-4-2/h3-19H2,1-2H3,(H,23,26)
InChi Key
FMFKQXKYWWJNJS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes.1 AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw.2 At concentrations as high as 30 µM, AX 048 does not inhibit COX activity or interfere with central cannabinoid receptor signaling.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dennis, E.A. Diversity of group types, regulation, and function of phospholipase A2. The Journal of Biological Chemisty 269(18), 13057-13060 (1994).

    2. Yaksh, T.L., Kokotos, G., Svensson, C.I., et alSystemic and intrathecal effects of a novel series of phospholipase A2 inhibitors on hyperalgesia and spinal prostaglandin E2 release. J. Pharmacol. Exp. Ther. 316(1), 466-475 (2006).