See personalized New Product recommendations! Get personalized New Product recommendations! Register or Login for personalized New Product recommendations!

Holiday Notification: Cayman Chemical will be closed Monday, May 28, 2012, in observance of the Memorial Day holiday. More…
Please feel free to continue placing orders via our website or via fax at 734-971-3640. You may send an email to customer service at custserv@caymanchem.com , or to technical support at techserv@caymanchem.com which we will respond to the next business day. Cayman will resume regular business hours and shipping schedules on Tuesday, May 29, 2012. Thank you for your patience and understanding.

Monoacylglycerol Lipase Inhibitor Screening Assay Kit

Cayman Chemical Item Number 705192

MAGL; MGL

Monoacylglycerol Lipase Inhibitor Screening Assay Kit

See more

Description

The endocannabinoid system is a ubiquitous lipid signaling system that is involved in various regulatory functions throughout the body. The main endocannabinoids are arachidonoyl ethanolamide (AEA) and 2-arachidonoyl glycerol (2-AG). They bind to G protein-coupled receptors, of which the cannabinoid (CB1) receptor is densely distributed in areas of the brain related to motor control, cognition, emotional responses, and homeostasis.1,2,3,4 Acting via the CB2 receptor in the peripheral tissues, the endocannabinoid system is one of the crucial modulators of the autonomic nervous system, the immune system, and microcirculation. Endocannabinoids are released upon demand from lipid precursors in a receptor-dependent manner. They are transported into cells by an apparently specific uptake system and degraded primarily by two enzymes, fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) resulting in the termination of their biological actions.5 FAAH, a serine hydrolase, can degrade many fatty acid amides, including AEA. Although FAAH can hydrolyze 2-AG, the main enzyme responsible for the inactivation of this monoglyceride is another serine hydrolase, MAGL. Finding inhibitors to these endocannabinoid hydrolases could offer another approach in the treatment of pain, obesity, and various neurological diseases, where higher endocannabinoid activity would be beneficial. An advantage of such enzyme inhibition over direct cannabinoid agonists could result in higher selectivity, as it would increase activity of the endocannabinoid system only at sites where on-going production of endocannabinoids is taking place.6 Cayman’s Monoacylglycerol Lipase Inhibitor Screening Assay provides a convenient method for screening human MAGL inhibitors. MAGL hydrolyzes 4-nitrophenylacetate resulting in a yellow product, 4-nitrophenol, with an absorbance of 405-412 nm.7

1 Stella, N., Schweitzer, P., and Piomelli, D. A second endogenous cannabinoid that modulates long-term potentiation. Nature 388 773-778 (1997).

2 Sugiura, T., Kodaka, T., Kondo, S., et al. 2-Arachidonoylglycerol, a putative endogenous cannabinoid receptor ligand, induces rapid, transient elevation of intracellular free Ca2+ in neuroblastoma X glioma hybrid NG108-15 cells. Biochem Biophys Res Commun 229 58-64 (1996).

3 Kondo, S., Kondo, H., Nakane, S., et al. 2-Arachidonoylglycerol, an endogenous cannabinoid receptor agonist: Identification as one of the major species of monoacylglycerols in various rat tissues, and evidence for its generation through Ca2+-dependent and -independent mechanisms. FEBS Lett 429 152-156 (1998).

4 Rodríguez De Fonseca, F., Del Arco, I., Bermudez-Silva, F., et al. The endocannabinoid system: Physiology and pharmacology. Alcohol Alcohol 40(1) 2-14 (2005).

5 Dinh, T.P., Carpenter, D., Leslie, F.M., et al. Brain monoglyceride lipase participating in endocannabinoid inactivation. Proc Natl Acad Sci USA 99(16) 10819-10824 (2002).

6 Lambert, D.M., and Fowler, C.J. The endocannabinoid system: Drug targets, lead compounds, and potential therapeutic applications. J Med Chem 48(16) 5059-5087 (2005).

7 Muccioli, G.G., Labar, G., and Lambert, D.M. CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay. ChemBioChem 9 2704-2710 (2008).

Synonyms
  • MAGL
  • MGL
Stability 1 year
Storage -80°C
Shipping Dry ice in continental US; may vary elsewhere

Background Reading

Stella, N., Schweitzer, P., and Piomelli, D. A second endogenous cannabinoid that modulates long-term potentiation. Nature 388 773-778 (1997).

Sugiura, T., Kodaka, T., Kondo, S., et al. 2-Arachidonoylglycerol, a putative endogenous cannabinoid receptor ligand, induces rapid, transient elevation of intracellular free Ca2+ in neuroblastoma X glioma hybrid NG108-15 cells. Biochem Biophys Res Commun 229 58-64 (1996).

Kondo, S., Kondo, H., Nakane, S., et al. 2-Arachidonoylglycerol, an endogenous cannabinoid receptor agonist: Identification as one of the major species of monoacylglycerols in various rat tissues, and evidence for its generation through Ca2+-dependent and -independent mechanisms. FEBS Lett 429 152-156 (1998).

Rodríguez De Fonseca, F., Del Arco, I., Bermudez-Silva, F., et al. The endocannabinoid system: Physiology and pharmacology. Alcohol Alcohol 40(1) 2-14 (2005).

Dinh, T.P., Carpenter, D., Leslie, F.M., et al. Brain monoglyceride lipase participating in endocannabinoid inactivation. Proc Natl Acad Sci USA 99(16) 10819-10824 (2002).

Lambert, D.M., and Fowler, C.J. The endocannabinoid system: Drug targets, lead compounds, and potential therapeutic applications. J Med Chem 48(16) 5059-5087 (2005).

Muccioli, G.G., Labar, G., and Lambert, D.M. CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay. ChemBioChem 9 2704-2710 (2008).

Show all 7 Hide all but first 3
705192-96well
96-Well Solid Plate (Colorimetric Assay)
MAGL Substrate 1 ea
MAGL (human recombinant) Assay Reagent 1 ea
MAGL Assay Buffer (10X) 1 ea
Size Price Quantity Subtotal
96 wells $280.00 $0.00
Bulk Contact
Cart Total $0.00

This product is also available to buy in bulk quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-05-26. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

You may be eligible to receive a free sample Monoacylglycerol Lipase Inhibitor Screening Assay Kit under the Cayman Challenge program.

Related Products

FAAH Inhibitor Screening Assay Kit
JZL 184
Monoacylglycerol Lipase Blocking Peptide
Monoacylglycerol Lipase Polyclonal Antibody
URB602
URB754
WWL70 Exclusive
Show all 7 Hide all but first 3

Downloads

Batch-specific Information

Login to access batch-specific information

Cayman Chemical is a manufacturer, supplier and vendor of biochemical reagents, assay kits, antibodies, and proteins.

Other Resources
Management Team Company Profile Company History ChemAssistant Tools FAQs Cayman Europe Cayman Pharma CaBRI Cayman Gear Press Releases Illustrations and Charts Key Research Area Posters Article Library Analysis Tools Conference Schedule Order Terms Browser Recommendation Privacy Statement Site Map

Cayman Chemical Company · 1180 East Ellsworth Road · Ann Arbor, Michigan 48108 · USA

Toll Free: (800) 364-9897 (USA and Canada Only) · Fax: (734) 971-3640

Copyright 2012 Cayman Chemical Company

Lost password?