ABX-1431CAS号: 1446817-84-0分子式: C20H22F9N3O2分子量: 507.39描述纯度储存/保存方法别名外观可溶性/溶解性In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
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纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
Elcubragistat
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外观 |
White solid
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可溶性/溶解性 |
DMSO : 125 mg/mL (246.36 mM; Need ultrasonic)
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生物活性 | |
In vitro(体外研究) |
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.
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In vivo(体内研究) |
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.
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