Description: 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 carcinoma model when administered at a dose of 3 mg/animal.

Name: Roxadustat-d5
CAS#: 2043026-13-5 (d5-labeled)
Chemical Formula: C19H11D5N2O5
Exact Mass: 357.1373
Molecular Weight: 357.3765
Elemental Analysis: C, 63.86; H, 5.92; N, 7.84; O, 22.38

Synonym: Roxadustat-d5; Roxadustat d5;

IUPAC/Chemical Name: (4-hydroxy-1-methyl-7-(phenoxy-d5)isoquinoline-3-carbonyl)glycine

InChi Key: YOZBGTLTNGAVFU-VIQYUKPQSA-N

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

SMILES Code: CC1=NC(C(NCC(O)=O)=O)=C(C2=C1C=C(C=C2)OC3=C(C([2H])=C(C([2H])=C3[2H])[2H])[2H])O

Appearance: Solid powder

Purity: >99% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001