N-Arachidonyl maleimide

• 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
• 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。

N-Arachidonyl maleimide名称

• 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

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
• 靶点实验:

  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
• InChIKey: GZNZRHSGGQUYAP-DOFZRALJSA-N
• SMILES: CCCCCC=CCC=CCC=CCC=CCCCCN1C(=O)C=CC1=O
• 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靶点实验

查看更多实验

实验名称：Inhibition of human recombinant MGL by liquid scintillation counting 来源：ChEMBL 靶标：Monoglyceride lipase External Id：CHEMBL1053085

实验名称：Discovery of Small Molecules to Inhibit Human Cytomegalovirus Nuclear Egress 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：HCMV UL50 External Id：HMS1262

实验名称：A screen for small molecules that modulate mitochondrial supercomplex formation 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：N/A External Id：HMS1482

实验名称：Selectivity ratio of IC50 for human FAAH to IC50 for human MGL 来源：ChEMBL 靶标：N/A External Id：CHEMBL1045639

实验名称：Cell-based high throughput primary assay to identify activators of GPR151 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_1X%ACT

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify inhibitors of... 来源：The Scripps Research Institute Molecular Screening Center External Id：MITF_INH_Alpha_1536_1X%INH PRUN

实验名称：Stabilization of p53 in human papillomavirus-positive cells 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：Cellular tumor antigen p53 External Id：HMS1485

实验名称：Discovering small molecule activators of G protein-gated inwardly-rectifying potassiu... 来源：15621 靶标：G protein-activated inward rectifier potassium channel 2 External Id：VANDERBILT_HTS_GIRK2_MPD

实验名称：Inhibition of [3H]2-OG binding to human MGL at 40 times IC50 treated for 1 hr before ... 来源：ChEMBL 靶标：Monoglyceride lipase External Id：CHEMBL1045648

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N-Arachidonyl maleimide英文别名

• 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