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CAS No.: 1446817-84-0

Elcubragistat Catalog No. CSN23660

Synonyms: ABX-1431

ABX-1431 works as both a cannabinoid receptor agonist and a MAGL inhibitor.

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生物活性

实验方案

技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9709 mL
- 9.8544 mL
- 19.7087 mL
- 5 mM
- 0.3942 mL
- 1.9709 mL
- 3.9417 mL
- 10 mM
- 0.1971 mL
- 0.9854 mL
- 1.9709 mL

技术信息

CAS号

1446817-84-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H22F9N3O2

运输

蓝冰

分子量

507.39

别名

ABX-1431

溶解度

DMSO	220.0 mg/mL (433.6 mM)
Water	insoluble

动物实验配方

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