ABX-1431
(Synonyms: ABX-1431) 目录号 : GC19412
An inhibitor of MAGL
Cas No.:1446817-84-0
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet