ABX-1431

製品コードS8823 バッチS882301

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C20H22F9N3O2
分子量 507.39 CAS No. 1446817-84-0
Solubility (25°C)* 体外 DMSO 100 mg/mL (197.08 mM)
Ethanol 100 mg/mL (197.08 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 ABX-1431 is a highly potent, selective, and CNS-penetrant Monoacylglycerol lipase (MGLL) inhibitor with IC50 values of 14 nM and 27 nM for hMGLL and mMGLL respectively.
in vitro

ABX-1431 is 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 min inhibitor incubation time causes 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. ABX-1431 inhibits MGLL via carbamoylation of the catalytic nucleophile Ser122[1].
in vivo

Pharmacokinetic analysis in rats and dogs of ABX-1431 indicate low to moderate systemic clearance, moderate volume of distribution, and high oral bioavailability (64% in rat, 57% in dog). While ABX-1431 is stable in human and dog plasma, it is not stable in rat plasma. ABX-1431 is a potent and selective inhibitor of MGLL in mouse and rat brain in vivo[1]. ABX-1431 inhibits MGLL activity with an ED50 of 0.5-1.4 mg/kg (po) and dose-dependently increases brain 2-AG levels in mouse brain. A rat inflammatory pain model is used to assess the pharmacodynamics effect. ABX-1431 demonstrates potent antinociceptive effects in a formalin paw test at a dose that produced near complete MGLL inhibition and maximal elevation of 2-AG[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 PC3 cells
濃度 0.1-10 μM
反応時間 30 min
実験の流れ

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 with compound for 30 min at 37°C with 5% CO2. Cells are washed, harvested, and lysed by probe sonication. Cell lysates (2 mg/mL) are treated with JW912 (1 μM) and analyzed by SDS-PAGE and in-gel fluorescence scanning.
動物実験 動物モデル male Sprague-Dawley rats
投薬量 1 mg/kg
投与方法 IV

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。