| CAS NO: | 876305-42-9 |
| 包装 | 价格(元) |
| 5mg (solution) | 电议 |
| 10mg (solution) | 电议 |
| 50mg (solution) | 电议 |
| Physical Appearance | A solution in ethanol. To change the solvent, simply evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice. |
| Storage | Store at -80°C |
| M.Wt | 369.5 |
| Cas No. | 876305-42-9 |
| Formula | C24H35NO2 |
| Synonyms | NAM |
| Solubility | ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | eicosa-5Z,8Z,11Z,14Z-tetraenyl-1-pyrrole-2,5-dione |
| Canonical SMILES | CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCCN1C(=O)C=CC1=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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