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Catalog Number | orb1739514 |
---|---|
Category | Small Molecules |
Description | Roxadustat-d5 |
CAS Number | 2043026-13-5 |
Purity | 0.98 |
MW | 357.37 |
SMILES | 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 |
Formula | C19H11D5N2O5 |
Biological Activity | 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...... |
Storage | -20°C |
Note | For research use only |
Expiration Date | 12 months from date of receipt. |