ABX-1431 _MAGL 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEABX-1431Cat. No.: HY-117632CAS No.: 1446817-84-0分式: CHFNO分量: 507.39作靶點(diǎn): MAGL作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg/mL (246.36 mM; Need ultrason

2、ic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.10 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.10 mM); Suspended solution; Need ultrasonic3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubili

3、ty: 2.08 mg/mL (4.10 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 ABX-1431種效，選擇性和服可的CNS-滲透性單酰 油脂肪酶 (MAGL)抑制劑，IC50 為14 nM。IC50 & Target IC50: 14 nM (human MGLL) 1體外研究 ABX-1431 is a potent human MGLL inhibitor (IC50=0.014 M) with 100-fold selectivity against ABHD6 and200-fold selectivity against PLA2G7.

4、ABX-1431 inhibits human PC3 cells with an IC50 of 0.0022 M. In thecell-based assay, 100-fold selectivity for MGLL over ABHD6 (IC50=0.253 M) and PLA2G7 (IC50=494 M)is maintained 1.體內(nèi)研究 ABX-1431 inhibits MGLL activity in rodent brain (ED50=0.5-1.4 mg/kg), increases brain 2-AG concentrations,and suppre

5、sses pain behavior in the rat formalin pain model 1.PROTOCOLCell Assay 1 Human prostate cancer PC3 cells are grown in F-12K medium supplemented with 10% fetal bovine serum at37C with 5% CO2 to 80% confluency in 100 mm dishes. ABX-1431 is added to cells to give finalconcentration of 0.1-10 M compound

6、 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 (1M) and analyzedby SDSand in-gel fluorescence scanning 1.MCE has not independently confirmed the accuracy of these methods. They are for refe

7、rence only.Animal Rats 1Administration 1 ABX-1431 is administered in a volume of 5 mL/kg. Male ICR mice or male Sprague Dawley rats 6 to 12weeks 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 ane

8、sthetized. Following blood collection, animals arekilled by decapitation and brains are removed, hemisected and frozen in liquid nitrogen for analysis 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Cisar JS, et al. Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment ofNeurological Disorders. J Med Chem. 2018 Oct 25;61(20):9062-9084.McePdfHeightCaution: Product has not been fully validated for medical appl