A pan HIF-PH inhibitor
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Enarodustat

Item No. 33785

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[7-hydroxy-5-(2-phenylethyl)[1,2,4]triazolo[1,5-a]pyridin-8-yl]carbonyl]-glycine
CAS Number
1262132-81-9
Synonyms
  • JTZ-951
Molecular Formula
C17H16N4O4
Formula Weight
340.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml
λmax
224 nm
SMILES
O=C(CNC(C1=C(C=C(CCC2=CC=CC=C2)N3N=CN=C13)O)=O)O
InChi Code
InChI=1S/C17H16N4O4/c22-13-8-12(7-6-11-4-2-1-3-5-11)21-16(19-10-20-21)15(13)17(25)18-9-14(23)24/h1-5,8,10,22H,6-7,9H2,(H,18,25)(H,23,24)
InChi Key
NALAUGMPMIVAOW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Enarodustat is a pan hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor (Kis = 16, 61, and 101 nM for HIF-PH1, -2, and -3, respectively).1 It increases erythropoietin (EPO) levels in Hep3B cells (EC50 = 4.7 µM). Enarodustat (3 mg/kg) increases plasma EPO levels in control rats, as well as plasma EPO and hemoglobin levels in 5/6-nephrectomized rats. It also decreases renal fatty acid and amino acid metabolism and increases renal glucose metabolism in streptozotocin-induced rat and alloxan-induced mouse models of diabetic nephropathy.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fukui, K., Shinozaki, Y., Kobayashi, H., et al. JTZ-951 (enarodustat), a hypoxia-inducibe factor prolyl hydroxylase inhibitor, stabilizes HIF-α protein and induces erythropoiesis without effects on the function of vascular endothelial growth factor. Eur. J. Pharmacol. 859, 172532 (2019).

    2. Hasegawa, S., Tanaka, T., Saito, T., et al. The oral hypoxia-inducible factor prolyl hydroxylase inhibitor enarodustat counteracts alterations in renal energy metabolism in the early stages of diabetic kidney disease. Kidney Int. 97(5), 934-950 (2020).