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. |