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N-Arachidonyl Maleimide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
N-Arachidonyl Maleimide图片
CAS NO:876305-42-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
N-Arachidonyl maleimide 是一种有效的、不可逆的单酰基甘油脂肪酶 (MAGL) 抑制剂,IC50 值为 140 nM。
Cas No.876305-42-9
别名N-花生四烯酸马来酰亚胺
化学名eicosa-5Z,8Z,11Z,14Z-tetraenyl-1-pyrrole-2,5-dione
Canonical SMILESCCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCCN1C(=O)C=CC1=O
分子式C24H35NO2
分子量369.5
溶解度≤30mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 140 nM

N-Arachidonyl Maleimide is a monoacylglycerol lipase (MGL) or MGL-like activity inhibitor.

2-Arachidonoyl glycerol (2-AG), an endogenous agonist of the central cannabinoid and peripheral cannabinoid receptors, is present with high levels in the central nervous system and is the most abundant molecular species of monoacylglycerol found brain. Monoacylglycerol lipase has been identified to hydrolyze 2-AG to arachidonic acid and glycerol, thereby terminating its biological actions.

In vitro: Previous study found that N-arachidonyl maleimide could increase the endogenous levels of 2-AG. Moreover, in agonist-stimulated guanosine 5'-O-(3-[(35)S]thio)triphosphate binding assay, N-arachidonyl maleimide was able to raise the potency of 2-AG, but not anandamide (AEA). In addition, unmasking of 2-AG effects of N-arachidonyl maleimide that were only partially reversed by SR141716A gave further support for the existence of non-CB(1), non-CB(2) cannabinoid receptors [1].

In vivo: Animal study showed that N-arachidonyl maleimide could unmask 2-AG activity in a tetrad of in vivo tests sensitive to the effects of cannabinoids in mice. The efficacy of 2-AG to produce hypothermia was reduced by the treatment of N-arachidonyl maleimide compared with Delta(9)-tetrahydrocannabinol. All tetrad effects were partially CB(1) receptor-mediated because they could be attenuated by CB(1) antagonist SR141716A and in CB(1)(-/-) mice [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Burston JJ 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.