| 7-hydroxycoumarinyl Arachidonatesubstrate for cPLA2 |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 161180-11-6 | SDF | Download SDF |
| Synonyms | Umbelliferyl Arachidonate | ||
| Chemical Name | 5Z,8Z,11Z,14Z-eicosatetraenoic acid, 2-oxo-2H-1-benzopyran-7-yl ester | ||
| Canonical SMILES | CCCCC/C=CC/C=CC/C=CC/C=CCCCC(=O)Oc1ccc2ccc(=O)oc2c1 | ||
| Formula | C29H36O4 | M.Wt | 448.6 |
| Solubility | ≤25mg/ml in DMSO;50mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A solution in ethanol | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
7-hydroxycoumarinyl-arachidonate (7-HCA), a fluorogenic substrate for monoacylglycerol lipase (MAGL), can be used with MAGL as a novel fluorescence-based assay to screen small molecule inhibitors of MAGL.
MAGL protein catalyzed the hydrolysis of 7-HCA to generate arachidonic acid and the highly fluorescent 7-hydroxyl coumarin (7-HC). 7-hydroxycoumarin (7-HC) can be monitored spectrophotometrically (excitation at 335 nm, emission at 450 nm). Release of 7-HC was measured using a fluorometer. MAGL protein catalyzed the hydrolysis of 7-HCA with an apparent Km of 9.8 μM and Vmax of 1.7 mmol/min/mg of protein. The assay is specific for MAGL as assay buffer alone or heat-denatured MAGL protein showed no significant activity against 7-HCA [1]. 7-hydroxycoumarinyl Arachidonate is the arachidonic acid ester of 7-hydroxycoumarin (umbelliferone) and can be used as a substrate for cPLA2. Hydrolysis of 7-hydroxycoumarinyl arachidonate by phospholipase resulted in the release of the fluorescent compound [2,3].
References:[1]. Wang Y, Chanda P, Jones P G, et al. A fluorescence-based assay for monoacylglycerol lipase compatible with inhibitor screening[J]. Assay and drug development technologies, 2008, 6(3): 387-393.[2]. Huang Z, Laliberte F, Tremblay N M, et al. A continuous fluorescence-based assay for the human high-molecular-weight cytosolic phospholipase A2[J]. Analytical biochemistry, 1994, 222(1): 110-115.[3]. Pickard R T, Chiou X G, Strifler B A, et al. Identification of essential residues for the catalytic function of 85-kDa cytosolic phospholipase A2 Probing the role of histidine, aspartic acid, cysteine, and arginine[J]. Journal of Biological Chemistry, 1996, 271(32): 19225-19231.
