Roxadustat-d5 - CAS 2043026-13-5

Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4, 1.26, and 1.32 μM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively) . It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases, including lysine-specific demethylase 5A (KDM5A), KDM5B, -5C, -5D, and -6B (IC50s = >100 μM for all) . Roxadustat (10-200 μM) stabilizes HIF-1α and HIF-2α in Hep3B hepatocellular carcinoma cells. It increases levels of secreted erythropoietin in Hep3B cells in a concentration-dependent manner and increases erythropoiesis in rats when administered at doses of 25 and 50 mg/kg. Roxadustat reverses anemia in a rat model of chronic inflammation induced by peptidoglycan-polysaccharide, as well as a rat model of chronic kidney disease induced by 5/6 nephrectomy. It reduces tumor growth and increases survival in a murine Lewis lung carcin......

Ferroptosis, HIF/HIF Prolyl-Hydroxylase

Chromatin/Epigenetic, Apoptosis, Metabolism

2043008

C19H11D5N2O5

357.37

CC=1C2=C(C(O)=C(C(NCC(O)=O)=O)N1)C=CC(OC3=C(C(=C(C(=C3[2H])[2H])[2H])[2H])[2H])=C2

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