N-Arachidonyl Maleimide
(Synonyms: N-花生四烯酸马来酰亚胺) 目录号 : GC10285
A potent inhibitor of monoacylglycerol lipase
Cas No.:876305-42-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 876305-42-9 | SDF | |
| 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 SMILES | CCCCC/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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7064 mL | 13.5318 mL | 27.0636 mL |
| 5 mM | 0.5413 mL | 2.7064 mL | 5.4127 mL |
| 10 mM | 0.2706 mL | 1.3532 mL | 2.7064 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。