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N-Arachidonyl maleimide

N-Arachidonyl maleimide用途

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。

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N-Arachidonyl maleimide名称

[ CAS 号 ]:
876305-42-9

[ 中文名 ]:
N-Arachidonyl Maleimide

[ 英文名 ]:
N-Arachidonyl maleimide

[英文别名 ]:

N-Arachidonyl maleimide生物活性

[ 描述 ]:

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。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> MAGL

研究领域 >> 代谢疾病

[ 靶点 ]

IC50: 140 nM (MAGL)[1]

[体外研究]

N-花生四烯基马来酰亚胺是一种公认的MAGL抑制剂,可用于调节2-花生四烯酸甘油(2-AG)的作用。N-花生四烯酸马来酰亚胺增加脑内2-AG的水平。N-花生四烯酸马来酰亚胺在相对低的浓度(IC50,140 nM)下阻止小脑膜介导的2-AG降解[1]。

[体内研究]

当与1 mg/kg剂量的N-花生四烯酸马来酰亚胺结合时,2-AG(1、3和10 mg/kg)产生显著的剂量依赖性低温、运动抑制、抗伤害和催化作用[1]。

[参考文献]

[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.

N-Arachidonyl maleimide物理化学性质

[ 密度 ]:
1.0±0.1 g/cm3

[ 沸点 ]:
492.9±34.0 °C at 760 mmHg

[ 分子式 ]:
C₂₄H₃₅NO₂

[ 分子量 ]:
369.540

[ 闪点 ]:
185.2±18.0 °C

[ 精确质量 ]:
369.266785

[ PSA ]:
37.38000

[ LogP ]:
7.89

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.524

[ 储存条件 ]:
-20°C，密闭，干燥

N-Arachidonyl maleimide安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H317

[ 警示性声明 ]:
P280

[ 危险品运输编码 ]:
NONH for all modes of transport

N-Arachidonyl maleimide文献

Crystal structure of the human monoacylglycerol lipase, a key actor in endocannabinoid signaling.

ChemBioChem. 11 , 218-27, (2010)

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 ...

Characterization of the sulfhydryl-sensitive site in the enzyme responsible for hydrolysis of 2-arachidonoyl-glycerol in rat cerebellar membranes.

Chem. Biol. 12 , 649-56, (2005)

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...

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