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Chemical Structure| 1446817-84-0 同义名 : ABX-1431
CAS号 : 1446817-84-0
货号 : A866363
分子式 : C20H22F9N3O2
纯度 : 99%+
分子量 : 507.393
MDL号 : MFCD31735112
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(492.71 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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