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ABX-1431 Sale

(Synonyms: ABX-1431) 目录号 : GC19412

An inhibitor of MAGL

ABX-1431 Chemical Structure

Cas No.:1446817-84-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥450.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

Human prostate cancer PC3 cells are grown in F-12K medium supplemented with 10% fetal bovine serum at 37°C with 5% CO2 to 80% confluency in 100 mm dishes. ABX-1431 is added to cells to give final concentration of 0.1-10 µM compound in serum free media. Cells are incubated for 30 min. Cells are washed, harvested, and lysed by probe sonication. Cell lysates (2mg/mL) are treated with JW912 (1µM) and analyzed by SDS-PAGE and in-gel fluorescence scanning[1].

Animal experiment:

Rats[1]ABX-1431 is administered in a volume of 5 mL/kg. Male ICR mice or male Sprague Dawley rats 6 to 12 weeks are administered single oral doses of ABX-1431 (0.5-32 mg/kg for mice and 0.03-10 mg/kg for rats). Four hours after ABX-1431 administration, animals are anesthetized. Following blood collection, animals are killed by decapitation and brains are removed, hemisected and frozen in liquid nitrogen for analysis[1].

References:

[1]. Cisar JS, et al. Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders. J Med Chem. 2018 Oct 25;61(20):9062-9084.

产品描述

ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.

ABX-1431 is a potent human MGLL inhibitor (IC50=0.014 µM) with >100-fold selectivity against ABHD6 and >200-fold selectivity against PLA2G7. ABX-1431 inhibits human PC3 cells with an IC50 of 0.0022 µM. In the cell-based assay, >100-fold selectivity for MGLL over ABHD6 (IC50=0.253 µM) and PLA2G7 (IC50=494 µM) is maintained[1].

ABX-1431 inhibits MGLL activity in rodent brain (ED50=0.5-1.4 mg/kg), increases brain 2-AG concentrations, and suppresses pain behavior in the rat formalin pain model[1].

[1]. Cisar JS, et al. Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders. J Med Chem. 2018 Oct 25;61(20):9062-9084.

Chemical Properties

Cas No. 1446817-84-0 SDF
别名 ABX-1431
Canonical SMILES O=C(N1CCN(CC2=CC=C(C(F)(F)F)C=C2N3CCCC3)CC1)OC(C(F)(F)F)C(F)(F)F
分子式 C20H22F9N3O2 分子量
溶解度 DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 mg/ml,Ethanol:PBS (pH 7.2) (1:10): 0.1 mg/ml 储存条件 Store at -20°C
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