Roxadustat (FG-4592) - CAS 808118-40-3
Catalog number: B0084-438323
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C19H16N2O5
Molecular Weight:
352.34
COA:
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Targets:
HIF/HIF Prolyl-Hydroxylase
Description:
Roxadustat (FG-4592) is an HIF α prolyl hydroxylase inhibitor, stabilizes HIF-2 and induces EPO production.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-438323 500 mg $198 In stock
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Purity:
>98%
MSDS:
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Application:
For research used only
1. Hypoxia-regulated mechanisms in the pathogenesis of obesity and non-alcoholic fatty liver disease
Sander Lefere • Christophe Van Steenkiste • Xavier Verhelst. Cell. Mol. Life Sci.
A relatively novel approach in modifying the hypoxia adaptive response in obesity and metabolic disease has focused on inhibition of PHDs, inspired by promising applications of PHD inhibitors (PHI) in animal models of anemia and ischemic disease. Two recently published clinical trials using the PHI roxadustat for anemia in chronic kidney disease show potential benefit, via upregulation of HIF-dependent genes in iron metabolism and hemoglobin synthesis. Trials investigating PHIs in coronary and peripheral vascular ischemia are underway.
2. Hypoxia-Inducible Factor Stabilizers: a New Avenue for Reducing BP While Helping Hemoglobin?
Farhanah Yousaf & Bruce Spinowitz. Curr Hypertens Rep (2016) 18: 23
Several pharmaceutical companies have filed new drug applications for the use of HIF-PHD inhibitor in the treatment of anemia. Fibrogen has completed phase II trials on FG-2216. However, human clinical trials investigating FG-2216 have not been conducted since 2007 when a case of death due to fulminant hepatitis was reported in a phase II trial, in spite of FDA’sapprovaltoresumeclinicalinvestigations. A second-generation HIF-PHD inhibitors, FG-4592 (roxadustat), with an improved pharmacokinetic and pharma-codynamic profile has now reached phase III trials. The phase II a trial investigating multiple doses of FG-4592 with BIWor TIW dosing frequency in CKD patients not on dialysis revealed a dose-related increase in hemoglobin from baseline while suppressing hepcidin levels.
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