1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVadadustatCat. No.: HY-101277CAS No.: 1000025-07-9Synonyms: PG-1016548; AKB-6548分式: CHClNO分量: 306.7作靶點(diǎn): 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 mon

2、th溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (326.05 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.2605 mL 16.3026 mL 32.6051 mL5 mM 0.6521 mL 3.2605 mL 6.5210 mL10 mM 0.3261 mL 1.6303 mL 3.2605 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Va

3、dadustat種新型的可滴定服的缺氧誘導(dǎo)因脯氨酰羥化酶 (HIF-PH) 抑制劑，前開發(fā)于治療貧。體外研究Vadadustat induces endogenous erythropoietin synthesis and enhances iron mobilization. Vadadustat iswell-tolerated in healthy volunteers and patients with chronic kidney disease, where it increases reticulocytes,1/2 Master of Small Molecules 您邊的抑

4、制劑師www.MedChemEplasma EPO, and Hb levels in a dose-dependent manner. The increase in plasma EPO levels seen withvadadustat is comparable in magnitude to that occurring physiologically at moderate altitude and shows anormal diurnal pattern with a return to baseline levels prior to the next dose. Vada

5、dustat improves ironhomeostasis by decreasing hepcidin and increasing transferrin levels. once-daily oral administration ofvadadustat, titrated to increase and maintain Hb in the target range, may provide multiple advantages overconventional ESAs 1. Vadadustat is observed to have a half-life of appr

6、oximately 4.5 hours. Overall,patients demonstrate an increase in Hb levels, from 9.91 g/dL at baseline to 10.54 g/dL by day 29. Ferritinlevels decrease from 334.1 ng/mL at baseline to 271.7 ng/mL by day 29 2.REFERENCES1. Pergola PE, et al. Vadadustat, a novel oral HIF stabilizer, provides effective

7、anemia treatment in nondialysis-dependent chronic kidneydisease. Kidney Int. 2016 Nov;90(5):1115-1122.2. Gupta N, et al. Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors: A Potential New Treatment for Anemia in Patients With CKD. AmJ Kidney Dis. 2017 Feb 24. pii: S0272-6386(17)30110-5.McePdfHeightCaution: Product has not been fully validated for medical applications.For research u