同义名 :	ABX-1431
	CAS号 :	1446817-84-0
	货号 :	A866363
	分子式 :	C20H22F9N3O2
	纯度 :	99%+
	分子量 :	507.39
	MDL号 :	MFCD31735112
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Monoacylglycerol lipase (MAGL) is a serine hydrolase enzyme responsible for controlling the content and signaling of the endogenous cannabinoid 2-arachidonoylglycerol (2-AG) in the central nervous system. MAGL is a critical point of regulation of both the endocannabinoid and eicosanoid signaling pathways in the CNS and select peripheral tissues. ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant MGLL inhibitor with an IC50 value of 14 nM. [1]. ABX-1431 demonstrated acceptable pharmacokinetics in rodents and dogs. It inhibited MGLL activity with an ED50 of 0.5–1.4 mg/kg (po) and dose-dependently increased brain 2-AG levels in mouse brain. ABX-1431 demonstrated potent antinociceptive effects in a formalin paw test at a dose that produced near complete MGLL inhibition and maximal elevation of 2-AG. Currently, ABX-1431 has entered phase 2 clinical trials and shows promising preliminary results in patients suffering from a neurological disease[2].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.97mL 0.39mL 0.20mL	9.85mL 1.97mL 0.99mL	19.71mL 3.94mL 1.97mL

参考文献

[1]Cisar JS, Weber OD, Clapper JR, et al. Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders. J Med Chem. 2018;61(20):9062‐9084 [2]Jiang M, van der Stelt M. Activity-Based Protein Profiling Delivers Selective Drug Candidate ABX-1431, a Monoacylglycerol Lipase Inhibitor, To Control Lipid Metabolism in Neurological Disorders. J Med Chem. 2018;61(20):9059‐9061