A2984
N-花生四烯基马来酰亚胺
≥98% (HPLC)
方案
≥98% (HPLC)
表单
solid
储存条件
under inert gas
储存温度
−20°C
SMILES字符串
CCCCC\C=C/C\C=C/C\C=C/C\C=C/CCCCN1C(=O)C=CC1=O
InChI
1S/C24H35NO2/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-22-25-23(26)20-21-24(25)27/h6-7,9-10,12-13,15-16,20-21H,2-5,8,11,14,17-19,22H2,1H3/b7-6-,10-9-,13-12-,16-15-
InChI key
GZNZRHSGGQUYAP-DOFZRALJSA-N
生化/生理作用
N-Arachidonylmaleidmide (NAM) is structurally similar to the MAGL substrate 2-AG and displays a high potency for inhibition of MAGL. It is thought that NAM binds MAGL at the substrate binding site and inhibits enzyme activity through the Michael addition reaction at the Cys201, and to a lesser extent Cys242, residue of MAGL. In cerebellar rat membranes, NAM inhibits MAGL-like activity with an IC50 of 140 nM.
N-Arachidonylmaleidmide, NAM, is a potent irreversible inhibitor of Monoacylglycerol Lipase (MAGL), the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG).
特点和优势
This compound is featured on the Cannabinoid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Susanna M Saario et al.
Chemistry & biology, 12(6), 649-656 (2005-06-25)
We have previously reported that the endocannabinoid, 2-arachidonoyl-glycerol (2-AG), is hydrolyzed in rat cerebellar membranes by monoglyceride lipase (MGL)-like enzymatic activity. The present study shows that, like MGL, 2-AG-degrading enzymatic activity is sensitive to inhibition by sulfhydryl-specific reagents. Inhibition studies
Geoffray Labar et al.
Chembiochem : a European journal of chemical biology, 11(2), 218-227 (2009-12-04)
2-Arachidonoylglycerol plays a major role in endocannabinoid signaling, and is tightly regulated by the monoacylglycerol lipase (MAGL). Here we report the crystal structure of human MAGL. The protein crystallizes as a dimer, and despite structural homologies to haloperoxidases and esterases
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