Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ABX-1431 (Elcubragistat) 是口服具有活力的、选择性CNS-渗透性单酰基甘油脂肪酶抑制剂,IC50=14 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 385 | 现货 | ||
10 mg | ¥ 625 | 现货 | ||
25 mg | ¥ 1,255 | 现货 | ||
50 mg | ¥ 1,995 | 现货 | ||
100 mg | ¥ 3,775 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 415 | 现货 |
产品描述 | ABX-1431 (Elcubragistat) is a selective and orally available CNS-penetrant monoacylglycerol lipase (MAGL/MGLL) inhibitor (IC50: 14 nM). |
靶点活性 | MGLL (mouse):27 nM, MGLL (human):14 nM |
体外活性 | ABX-1431 was a potent human MGLL inhibitor (average IC50 = 0.014 μM) with >100-fold selectivity against ABHD6 and >200-fold selectivity against PLA2G7. Treatment of intact human PC3 cells with ABX-1431 following a 30-minute inhibitor incubation time caused concentration-dependent inhibition of MGLL activity with an IC50 value of 0.0022 μM, which is ~6-fold more potent than that observed in vitro. In the cell-based assay, >100-fold selectivity for MGLL over ABHD6 (IC50 = 0.253 μM) and PLA2G7 (IC50 = 494 μM) was maintained. |
体内活性 | In vivo, 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. |
细胞实验 | Human prostate cancer PC3 cells were 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 was added to cells to give final concentration of 0.1–10 μM compound in serum free media. Cells were incubated with compound for 30 min at 37°C with 5% CO2. Cells were washed, harvested, and lysed by probe sonication. Cell lysates (2mg/mL) were treated with JW912 (1μM) and analyzed by SDS-PAGE and in-gel fluorescence scanning. |
动物实验 | All animals were 6?8 weeks old at the time of study and weighed between 197-217 g. Animals (n = 3 per dosing route) were dosed with ABX-1431 at 1 mg/kg iv (in 70% polyethylene glycol (PEG) 400 in hydroxypropyl-?-cylcodextran (HPBCD) in saline) or 5 mg/kg po (in 70% PEG 400 in 0.5% carboxymethylcellulose (CMC, w/v) in saline). Animals were fasted overnight, and food withheld until 4 h post dose. Approximately 100 μL of blood were collected via a jugular vein catheter at 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h after intravenous and 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h after oral administration. All blood samples were collected into tubes containing 400 μL acetonitrile to immediately inactivate blood esterase activity and frozen at ?80 °C. Samples were thawed and centrifuged (14,000 rpm for 5 min at 4 °C) and the supernatant transferred for LCMS analysis. |
别名 | Elcubragistat |
分子量 | 507.39 |
分子式 | C20H22F9N3O2 |
CAS No. | 1446817-84-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 10 mg/mL (19.71 mM)
DMSO: 55 mg/mL (108.4 mM), Sonication is recommended.
H2O: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.9709 mL | 9.8544 mL | 19.7087 mL | 49.2718 mL |
5 mM | 0.3942 mL | 1.9709 mL | 3.9417 mL | 9.8544 mL | |
10 mM | 0.1971 mL | 0.9854 mL | 1.9709 mL | 4.9272 mL | |
DMSO | 20 mM | 0.0985 mL | 0.4927 mL | 0.9854 mL | 2.4636 mL |
50 mM | 0.0394 mL | 0.1971 mL | 0.3942 mL | 0.9854 mL | |
100 mM | 0.0197 mL | 0.0985 mL | 0.1971 mL | 0.4927 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
ABX-1431 1446817-84-0 Metabolism Lipase ABX1431 inhibit Monoacylglycerol lipase MAGL Elcubragistat ABX 1431 Inhibitor inhibitor