PeptideDB

N-Arachidonyl maleimide

CAS: 876305-42-9 F: C24H35NO2 W: 369.54

N-Arachidonyl maleimide is a potent, irreversible inhibitor of monoacylglycerol lipase (MAGL) with an IC50 value of 140
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Bioactivity N-Arachidonyl maleimide is a potent, irreversible inhibitor of monoacylglycerol lipase (MAGL) with an IC50 value of 140 nM[1].
Target IC50: 140 nM (MAGL)
Invitro N-Arachidonyl maleimide is a putative MAGL inhibitor, which can be used for modulation of the effects of 2-arachidonyl glycerol (2-AG). N-Arachidonyl maleimide increases endogenous levels of 2-AG in the brain. N-Arachidonyl maleimide prevents cerebellar membrane-mediated degradation of 2-AG at a relatively low concentration (IC50, 140 nM)[1].
In Vivo When combined with a 1 mg/kg dose of N-Arachidonyl maleimide, 2-AG (1, 3, and 10 mg/kg) produces significant and dose-dependent hypothermia, inhibition of locomotor activity, antinociception, and catalepsy[1].
Name N-Arachidonyl maleimide
CAS 876305-42-9
Formula C24H35NO2
Molar Mass 369.54
Appearance Liquid
Transport Room temperature in continental US; may vary elsewhere.
Storage

-80°C

Reference [1]. Susanna M Saario, et al. Characterization of the Sulfhydryl-Sensitive Site in the Enzyme Responsible for Hydrolysis of 2-arachidonoyl-glycerol in Rat Cerebellar Membranes. Chem Biol. 2005 Jun;12(6):649-56. [2]. James J Burston, et al. N-arachidonyl Maleimide Potentiates the Pharmacological and Biochemical Effects of the Endocannabinoid 2-arachidonylglycerol Through Inhibition of Monoacylglycerol Lipase. J Pharmacol Exp Ther. 2008 Nov;327(2):546-53.