The quantity field is empty. Please enter a quantity of 1 or more to add items to your cart.
Description
Overview
A cell-permeable hexanoate ester compound that acts as a potent, selective, non-competitive, and reversible inhibitor of monoacylglycerol lipase (MAGL, Ki = 400 nM, IC50 = 240 nM for hydrolysis of 2- arachidonoylglycerol (2-AG). Displays good selectivity over a broad panel of related enzymes and does not bind to CB1 and CB2 cannabinoid receptors (Ki >10 µM). Shown to inhibit mouse brain MAGL (IC50 = 180 nM), but does not affect the activity of fatty acid amide hydrolaase (FAAH; IC50 = 59 µM) in any significant manner. Improves the course of experimental autoimmune encephalitis (EAE) murine model of multiple sclerosis (5 mg/kg/day, i.p. for 21 days) without inducing any undesirable CB1-agonist-like activity.
Catalogue Number
533088
Brand Family
Calbiochem®
Synonyms
MAGL Inhibitor, Cpd21
References
References
Hernandez-Torres, G., et al. 2014. Angew Chem Int Ed Engl.53, in press.
Hernandez-Torres, G., et al. 2014. Angew Chem Int Ed Engl.53, in press.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
01-March-2016 JSW
Synonyms
MAGL Inhibitor, Cpd21
Description
A cell-permeable hexanoate ester compound that acts as a potent, selective, non-competitive, and reversible inhibitor of monoacylglycerol lipase (MAGL, Ki = 400 nM, IC50 = 240 nM for hydrolysis of 2- arachidonoylglycerol (2-AG). Displays good selectivity over a broad panel of related enzymes and does not bind to CB1 and CB2 cannabinoid receptors (Ki >10 µM). Shown to inhibit mouse brain MAGL (IC50 = 180 nM), but does not affect the activity of fatty acid amide hydrolaase (FAAH; IC50 = 59 µM) in any significant manner. Improves the course of experimental autoimmune encephalitis (EAE) murine model of multiple sclerosis (5 mg/kg/day, i.p. for 21 days) without inducing any undesirable CB1-agonist-like activity.
Form
Off-white solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₆H₂₆O₄
Purity
≥98% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Hernandez-Torres, G., et al. 2014. Angew Chem Int Ed Engl.53, in press.