7-hydroxycoumarinyl Arachidonate (Synonyms: Umbelliferyl Arachidonate) |
| Catalog No.GC10565 |
substrate for cPLA2
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 161180-11-6
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
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.
| Cas No. | 161180-11-6 | SDF | |
| Synonyms | Umbelliferyl Arachidonate | ||
| Chemical Name | 5Z,8Z,11Z,14Z-eicosatetraenoic acid, 2-oxo-2H-1-benzopyran-7-yl ester | ||
| Canonical SMILES | CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)Oc1ccc2ccc(=O)oc2c1 | ||
| Formula | C29H36O4 | M.Wt | 448.6 |
| Solubility | DMF: >50 mg/ml,DMSO: >25 mg/ml,Ethanol: >100 mg/ml,Ethanol:PBS (1:1): 50 µg/ml | Storage | Store at -20°C, protect from light |
| 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 | 2.2292 mL | 11.1458 mL | 22.2916 mL |
| 5 mM | 0.4458 mL | 2.2292 mL | 4.4583 mL |
| 10 mM | 0.2229 mL | 1.1146 mL | 2.2292 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 35 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 *