1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. Molidustat sodium

Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia.

For research use only. We do not sell to patients.

CAS No. : 1375799-59-9

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Top Publications Citing Use of Products

    Molidustat sodium purchased from MedChemExpress. Usage Cited in: Drug Test Anal. 2025 May;17(5):647-654.  [Abstract]

    Beard hair chromatogram. Molidustat concentration is 55 pg/mg. From bottom to top: Transition for internal standard testosterone-d3 (292.24 > 96.99) and two transitions of molidustat (315.0 > 137.10 and 315.10 > 207.00).

    Molidustat sodium purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 3;503(1):297-303.  [Abstract]

    Effects of adaptaquin (10 mM) and Molidustat (10 mM) on Fe-8HQ (15 mM, 14 h)-induced LDH release in AML 12 cells.

    Molidustat sodium purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 3;503(1):297-303.  [Abstract]

    Morphology of HT-1080 cells treated with Fe-8HQ (10 mM, 8 h) ± adaptaquin (10 mM) or Molidustat (10 mM).

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    Description

    Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia[1][2].

    IC50 & Target

    IC50: 480 nM (PHD1), 280 nM (PHD2), 450 nM (PHD3)[1]

    Cellular Effect
    Cell Line Type Value Description References
    Sf9 IC50
    0.28 μM
    Compound: 22; BAY-85-3934
    Inhibition of recombinant human HIF-PHD2 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
    Inhibition of recombinant human HIF-PHD2 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
    10.1039/C6MD00240D
    Sf9 IC50
    0.45 μM
    Compound: 22; BAY-85-3934
    Inhibition of recombinant human HIF-PHD3 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
    Inhibition of recombinant human HIF-PHD3 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
    10.1039/C6MD00240D
    Sf9 IC50
    0.48 μM
    Compound: 22; BAY-85-3934
    Inhibition of recombinant human HIF-PHD1 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
    Inhibition of recombinant human HIF-PHD1 expressed in insect Sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate after 60 mins by DELFIA
    10.1039/C6MD00240D
    In Vitro

    Molidustat sodium (5 μM; 20 min) is sufficient to induce detectable levels of HIF-1α in HeLa cells. In a cell reporter assay, Molidustat sodium induces expression of a firefly luciferase reporter gene under the control of a hypoxia response element promoter with a mean (± SD) EC50 of 8.4 μM (n=4)[1]

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Molidustat sodium, by stabilizing the hypoxia-inducible factor (HIF), leads to a dose-dependent increase in erythropoietin (EPO) in both Wistar rats (0.5-5 mg/kg; oral; once daily for 26 days) and cynomolgus monkeys (0.5-1.5mg/kg; once daily for 5 days)[1].
    Molidustat sodium (0.5-10 mg/kg; orally; five times weekly) can normalize the blood pressure in rat models of chronic kidney disease (CKD) and effectively alleviate renal anemia in rats with impaired renal function[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    336.28

    Formula

    C13H13N8NaO2

    CAS No.
    SMILES

    [Na]OC1=C(N2N=NC=C2)C=NN1C3=NC=NC(N4CCOCC4)=C3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Purity & Documentation
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
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