Elcubragistat (Synonyms: ABX-1431)
目录号: PL06910 纯度: ≥99%
CAS No. :1446817-84-0
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中文名称
Elcubragistat
中文别名
1,1,1,3,3,3-六氟丙-2-基 4-(2-吡咯烷-1-基)-4-(三氟甲基)苄基)哌嗪-1-羧酸酯
英文名称
Elcubragistat
英文别名
ABX-1431;Elcubragistat
Cas No.
1446817-84-0
分子式
C20H22F9N3O2
分子量
507.39
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Elcubragistat (ABX-1431) 是一种高效,选择性和口服可用的 CNS-渗透性单酰基甘油脂肪酶 (MAGL) 抑制剂,IC50 为 14 nM。
生物活性
Elcubragistat (ABX-1431) is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC 50 of 14 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 14 nM (human MGLL)
体外研究(In Vitro)
Elcubragistat (ABX-1431) is a potent human MGLL inhibitor (IC50=0.014 μM) with >100-fold selectivity against ABHD6 and >200-fold selectivity against PLA2G7. Elcubragistat 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Elcubragistat (ABX-1431) inhibits MGLL activity in rodent brain (ED 50 =0.5-1.4 mg/kg), increases brain 2-AG concentrations, and suppresses pain behavior in the rat formalin pain model. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 125 mg/mL (246.36 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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