N-Arachidonyl maleimide

更新时间：2024-01-08 18:14:21

N-Arachidonyl maleimide结构式	常用名	N-Arachidonyl maleimide	英文名	N-Arachidonyl maleimide
	CAS号	876305-42-9	分子量	369.540
	密度	1.0±0.1 g/cm3	沸点	492.9±34.0 °C at 760 mmHg
	分子式	C₂₄H₃₅NO₂	熔点	N/A
	MSDS	中文版美版	闪点	185.2±18.0 °C
	符号	GHS07	信号词	Warning

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。

中文名	N-Arachidonyl Maleimide
英文名	N-Arachidonyl maleimide,1-(5Z,8Z,11Z,14Z)-5,8,11,14-Eicosatetraen-1-yl-1H-pyrrole-2,5-dione
英文别名	更多

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.

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

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

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...

1H-Pyrrole-2,5-dione, 1-[(5Z,8Z,11Z,14Z)-5,8,11,14-eicosatetraen-1-yl]-

1-[(5Z,8Z,11Z,14Z)-Icosa-5,8,11,14-tetraen-1-yl]-1H-pyrrole-2,5-dione

1-[(5Z,8Z,11Z,14Z)-5,8,11,14-Icosatetraen-1-yl]-1H-pyrrole-2,5-dione