A HIF-PH1, -2, and -3 inhibitor
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Daprodustat

Item No. 19915

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1,3-dicyclohexylhexahydro-2,4,6-trioxo-5-pyrimidinyl)carbonyl]-glycine
CAS Number
960539-70-2
Synonyms
  • GSK1278863
Molecular Formula
C19H27N3O6
Formula Weight
393.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 3 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 1 mg/ml
λmax
210, 265 nm
SMILES
O=C(N(C(C1C(NCC(O)=O)=O)=O)C2CCCCC2)N(C3CCCCC3)C1=O
InChi Code
InChI=1S/C19H27N3O6/c23-14(24)11-20-16(25)15-17(26)21(12-7-3-1-4-8-12)19(28)22(18(15)27)13-9-5-2-6-10-13/h12-13,15H,1-11H2,(H,20,25)(H,23,24)
InChi Key
RUEYEZADQJCKGV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $288

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    25 mg

    $587

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    Product Description

    Daprodustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 1 (HIF-PH1), HIF-PH2, and HIF-PH3 (IC50s = 3.5, 22.2, 5.5 nM, respectively).1 It is selective for HIF-PH1, -2, and -3 over factor-inhibiting HIF (FIH) and collagen prolyl hydroxylase (CP4H; IC50s = 9,800 and >200,000 nM, respectively). Daprodustat (25 and 50 µM) induces accumulation of HIF-1α and HIF-2α in Hep3B cells. In vivo, daprodustat (60 mg/kg) increases plasma levels of erythropoietin (EPO) in mice. It increases the number of reticulocytes and levels of hemoglobin in mice when administered at doses of 3, 10, and 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Aziazi, J.L., Duffy, K.J., Adms, D.F., et al. Discovery and preclinical characterization of GSK1278863 (daprodustat), a small molecule hypoxia inducible factor-prolyl hydroxylase inhibitor for anemia. J. Pharmacol. Exp. Ther. 363(347), 336-347 (2017).