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MJN110

MJN110用途

MJN110 是有效的,选择性单酰基甘油脂肪酶 (MAGL) 抑制剂。MJN110 减少肝巨噬细胞数量和炎性基因表达,并减慢纤维化进程。

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MJN110名称

[ CAS 号 ]:
1438416-21-7

[ 英文名 ]:
MJN110

[英文别名 ]:

MJN110

MJN110生物活性

[ 描述 ]:

MJN110 是有效的,选择性单酰基甘油脂肪酶 (MAGL) 抑制剂。MJN110 减少肝巨噬细胞数量和炎性基因表达,并减慢纤维化进程。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> MAGL

研究领域 >> 炎症/免疫

[体内研究]

MJN110(i.p.；0.0818mg/kg；每天两次,持续5.5天)以剂量依赖性方式逆转慢性收缩损伤(CCI)诱导的机械异常性疼痛和热痛觉过敏。各自的ED50值(95％置信限)为0.430(0.233-0.793)mg/kg[1]。动物模型：雄性C57BL/6J小鼠18至35g[1]剂量：0.0818mg/kg给药：I.p.；每日两次,持续5.5天。结果：以剂量依赖性方式逆转CCI诱导的机械异常性疼痛和热痛觉过敏。

[参考文献]

[1]. Wilkerson JL, et al. The Selective Monoacylglycerol Lipase Inhibitor MJN110 Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model. J Pharmacol Exp Ther. 2016 Apr;357(1):145-56.

[2]. Habib A, et al. Inhibition of monoacylglycerol lipase, an anti-inflammatory and antifibrogenic strategy in the liver. Gut. 2018 Oct 9. pii: gutjnl-2018-316137.

MJN110物理化学性质

[ 密度 ]:
1.47±0.1 g/cm3

[ 沸点 ]:
561.5±60.0 °C

[ 分子式 ]:
C₂₂H₂₁Cl₂N₃O₄

[ 分子量 ]:
462.32600

[ 精确质量 ]:
461.09100

[ PSA ]:
70.16000

[ LogP ]:
3.71470

[ 外观性状 ]:
粉末

[ 储存条件 ]:
室温，干燥，密封

MJN110安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
22-50/53

[ 安全声明 (欧洲) ]:
26-60-61

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

MJN110文献

Effect of selective inhibition of monoacylglycerol lipase (MAGL) on acute nausea, anticipatory nausea, and vomiting in rats and Suncus murinus.

Psychopharmacol. Ser. 232(3) , 583-93, (2015)

To determine the role of the endocannabinoid, 2-arachodonyl glycerol (2-AG), in the regulation of nausea and vomiting.We evaluated the effectiveness of the potent selective monoacylglycerol lipase (MA...

Proteome-wide reactivity profiling identifies diverse carbamate chemotypes tuned for serine hydrolase inhibition.

ACS Chem. Biol. , (2013)

Serine hydrolases are one of the largest and most diverse enzyme classes in Nature. Inhibitors of serine hydrolases are used to treat many diseases, including obesity, diabetes, cognitive dementia, an...

Evaluation of NHS carbamates as a potent and selective class of endocannabinoid hydrolase inhibitors.

ACS Chem. Neurosci. 4(9) , 1322-32, (2013)

Monoacylglycerol lipase (MAGL) is a principal metabolic enzyme responsible for hydrolyzing the endogenous cannabinoid (endocannabinoid) 2-arachidonoylglycerol (2-AG). Selective inhibitors of MAGL offe...

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