Roxadustat-FG-4592-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERoxadustatCat. No.: HY-13426CAS No.: 808118-40-3Synonyms: FG-4592分式: CHNO分量: 352.34作靶點: HIF/HIF Prolyl-Hydroxylase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)體外實驗 DMSO

2、 : 100 mg/mL (283.82 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.10 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (7.10 mM); Precipitated solution; Need ultrasonic3. 請依序添加每種溶劑： 10% DMS

3、O 90% corn oilSolubility: 2.5 mg/mL (7.10 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Roxadustat種服低氧誘導(dǎo)因脯氨酰羥化酶抑制劑 (HIF-PHI)，通過增加內(nèi) 性促紅細(xì)胞成素、改善鐵調(diào)節(jié)和降低鐵調(diào)素來促進(jìn)紅細(xì)胞成 1。IC50 & Target Hypoxia-inducible factor prolyl-hydroxylase 1體外研究 Roxadustat (5-50 M; 6 hours) significantly inhibits TBHP-induced apoptosis in PC

4、12 cells 2.Roxadustat (50 M; 6 hours) stabilizes HIF-1 protein expression in PC12 cells 2.Apoptosis Analysis 2Cell Line: PC12 cellsConcentration: 5, 20, 50 MIncubation Time: 6 hoursResult: Significantly inhibited TBHP-induced apoptosis.Western Blot Analysis 2Cell Line: PC12 cellsConcentration: 50 MI

5、ncubation Time: 6 hoursResult: stabilized HIF-1 protein expression.體內(nèi)研究 Roxadustat (50 mg/kg; i.p.; daily for 7 days) protects the survival of motor neurons and improves recoveryfrom spinal cord injury 2.Animal Model: 12-week female C57BL/6 mice 2Dosage: 50 mg/kgAdministration: Intraperitoneal injec

6、tion; daily for 7 daysResult: Protected the survival of motor neurons and improved recovery from spinal cord injury.戶使本產(chǎn)品發(fā)表的科研獻(xiàn)2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Science. 2016 Apr 1;352(6281):54-61. Cell Metab. 2017 Jan 10;25(1):73-85. Patent. US20180263995A1.See more customer validat

7、ions on HYPERLINK / www.MedChemEREFERENCES1. Provenzano R, et al. Roxadustat (FG-4592) Versus Epoetin Alfa for Anemia in Patients Receiving MaintenanceHemodialysis: A Phase2, Randomized, 6- to 19-Week, Open-Label, Active-Comparator, Dose-Ranging, Safety and Exploratory Efficacy Study. Am J Kidney Dis.2016 Jun;67(6):912-24.2. Wu K, et al. Stabilization of HIF-1 by FG-4592 promotes functional recovery and neural protection in experimental spinal cord injury.Brain Res. 2016 Feb 1;1632:19-26.McePdfHeightCaution: Product has not been fully validated for medical applications.For