An internal standard for the quantification of roxadustat
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Roxadustat-d5

Item No. 34235

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A solid
Solubility(Learn about Variance in Solubility)
Acetone: solubleDMSO: 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $502

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    Product Description

    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).1 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.2 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.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yeh, T.-L., Leissing, T.M., Abboud, M.I., et al. Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials. Chem. Sci. 8(11), 7651-7668 (2017).

    2. Del Balzo, U., Signore, P.E., Walkinshaw, G., et al. Nonclinical characterization of the hypoxia-inducible factor prolyl hydroxylase inhibitor roxadustat, a novel treatment of anemia of chronic kidney disease. J. Pharmacol. Exp. Ther. 374(4), 342-353 (2020).

    3. Nishide, S., Matsunaga, S., Shiota, M., et al. Controlling the phenotype of tumor-infiltrating macrophages via the PHD-HIF axis inhibits tumor growth in a mouse model. iScience 19, 940-954 (2019).