Roxadustat-d5

Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat (Cay-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). 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-1alpha and HIF-2alpha 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 carcinoma model when administered at a dose of 3 mg/animal.Formal Name: N-[(4-hydroxy-1-methyl-7-phenoxy-d5-3-isoquinolinyl)carbonyl]-glycine. CAS Number: 2043026-13-5. Molecular Formula: C19H11D5N2O5. Formula Weight: 357.4. Purity: >99% deuterated forms (d1-d5). Formulation: (Request formulation change), A solid. Solubility: Acetone: soluble, DMSO: soluble. SMILES: CC1=NC(C(NCC(O)=O)=O)=C(O)C2=C1C=C(OC3=C([2H])C([2H])=C([2H])C([2H])=C3[2H])C=C2. InChi Code: InChI=1S/C19H16N2O5/c1-11-15-9-13(26-12-5-3-2-4-6-12)7-8-14(15)18(24)17(21-11)19(25)20-10-16(22)23/h2-9,24H,10H2,1H3,(H,20,25)(H,22,23)/i2D,3D,4D,5D,6D. InChi Key: YOZBGTLTNGAVFU-VIQYUKPQSA-N.