An internal standard for the quantification of vadadustat
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Unlabeled Version(s)
15295Vadadustat
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Vadadustat-d5

Item No. 45871

Technical Information
Formal Name
N-[[5-(3-chlorophenyl-2,4,6-d3)-3-hydroxy-2-pyridinyl]carbonyl]-glycine-2,2-d2
CAS Number
2229917-78-4
Molecular Formula
C14H6ClD5N2O4
Formula Weight
Purity
≥95%
A 1 mg/ml solution in ethanol
Ethanol: Soluble
SMILES
OC1=CC(C(C([2H])=CC([2H])=C2Cl)=C2[2H])=CN=C1C(NC([2H])(C(O)=O)[2H])=O
InChi Code
InChI=1S/C14H11ClN2O4/c15-10-3-1-2-8(4-10)9-5-11(18)13(16-6-9)14(21)17-7-12(19)20/h1-6,18H,7H2,(H,17,21)(H,19,20)/i2D,3D,4D,7D2
InChi Key
JGRXMPYUTJLTKT-AWLPUSBPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Vadadustat-d5 is intended for use as an internal standard for the quantification of vadadustat (Item No. 15295) by GC- or LC-MS. Vadadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 1 (HIF-PH1), HIF-PH2, and HIF-PH3 (Kis = 0.19, 0.26, and 0.56 nM, respectively).1 It stabilizes HIF-1α and HIF-2α in Hep3B cells and human umbilical vein endothelial cells (HUVECs). Vadadustat selectively induces erythropoietin (EPO) over VEGF secretion in Hep3B cells. It increases red blood cell indices in a 5/6 nephrectomy-induced rat model of chronic kidney disease when administered at a dose of 90 mg/kg. Vadadustat (40 µM) inhibits proliferation in the mixed lymphocyte reaction in isolated human peripheral blood mononuclear cells (PBMCs).2 Formulations containing vadadustat have been used in the treatment of anemia in patients with chronic kidney disease.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zuk, A., Si, Z., Loi, S., et alPreclinical characterization of vadadustat (AKB-6548), an oral small molecule hypoxia-inducible factor prolyl-4-hydroxylase inhibitor, for the potential treatment of renal anemia. J. Pharmacol. Exp. Ther. 383(1), 11-24 (2022).

    2. Zielniok, K., Burdzinska, A., Kaleta, B., et alVadadustat, a HIF prolyl hydroxylase inhibitor, improves immunomodulatory properties of human mesenchymal stromal cells. Cells 9(11), 2396 (2020).