DO-264 - MAGL 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDO-264Cat. No.: HY-114157CAS No.: 2301866-59-9分式: CHClFNOS分量: 558.4作靶点: MAGL作通路: Metabolic Enzyme/Protease储存式: -20C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶解性数据体外实验 DMSO : 100 mg

2、/mL (179.08 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.72 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.72 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 DO-264个具有体内活性的、解酶结构域 12 (ABHD12) 的抑制剂，其 IC5

3、0 值为 11 nM。IC50 & Target IC50: 11 nM (ABHD12) 1.体外研究 DO-264 displays an IC50 value of 11 nM (9.6 nM-13 nM). DO-264 blocks lyso-PS hydrolysis activities ofrecombinant mouse and human ABHD12 in transfected HEK293T cell lysates (DO-264 IC50 values of 30and 90 nM against mouse and human ABHD12, respecti

4、vely) and the ABHD12-dependent lyso-PS lipaseactivity of membrane lysates from mouse brain (IC50=2.8 nM, 2.4 nM-3.3 nM) and human THP-1 cells(IC50= 8.6 nM, 6.3 nM-12 nM) 1.体内研究 Mice treated with DO-264 display dose-dependent increases in brain lyso-PS and 20:4 PS content that arequalitatively simila

5、r to the changes observed in ABHD12/ mice. DO-264-treated mice, however, showminimal impairment in auditory function following four weeks of drug exposure. Both ABHD12/ and DO-264-treated mice display exacerbated immunopathology following infection with the lymphocyticchoriomeningitis virus (LCMV) c

6、lone 13, resulting in severe inflammatory lung damage, heightenedchemokine production, and, in some cases, death 1.REFERENCES1. Ogasawara D, et al. Selective blockade of the lyso-PS lipase ABHD12 stimulates immune responses in vivo. Nat Chem Biol. 2018Dec;14(12):1099-1108.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400