Shelf life (days): 1460.0
Formulation: A solid
Formal Name: N-[(4-hydroxy-1-methyl-7-phenoxy-d5-3-isoquinolinyl)carbonyl]-glycine
Purity: ≥99% deuterated forms (d1-d5)
Formula Markup: C19H11D5N2O5
Formula Weight: 357.37112
CAS Number: 2043026-13-5
Notes: Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat (Item No. 15294) 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).{58503} 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.{58504} 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 carcinoma model when administered at a dose of 3 mg/animal.{58505}
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