A HIF-PH inhibitor
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Labeled Version(s)
45871Vadadustat-d5
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Vadadustat

Item No. 15295

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[5-(3-chlorophenyl)-3-hydroxy-2-pyridinyl]carbonyl]-glycine
CAS Number
1000025-07-9
Synonyms
  • AKB6548
  • PG-1016548
Molecular Formula
C14H11ClN2O4
Formula Weight
306.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:20): 0.04 mg/mlDMSO: 2 mg/mlEthanol: 2 mg/ml
λmax
262, 317 nm
SMILES
ClC1=CC=CC(C2=CC(O)=C(C(NCC(O)=O)=O)N=C2)=C1
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)
InChi Key
JGRXMPYUTJLTKT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    25 mg

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    50 mg

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    Cayman Chemical
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    Product Description

    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 al. Preclinical 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 al. Vadadustat, a HIF prolyl hydroxylase inhibitor, improves immunomodulatory properties of human mesenchymal stromal cells. Cells 9(11), 2396 (2020).