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

Molidustat (BAY 85-3934) 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 can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia.

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

CAS No. : 1154028-82-6

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Molidustat:

Molidustat Related Antibodies

Top Publications Citing Use of Products

    Molidustat 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 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 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).

    View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

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    HIF-1α HIF

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Molidustat (BAY 85-3934) 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 can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia[1][2].

    IC50 & Target

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

    Molidustat (BAY 85-3934) (5 μM; 20 min) is sufficient to induce detectable levels of HIF-1α in HeLa cells. In a cell reporter assay, Molidustat 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.

    Molidustat Related Antibodies
    In Vivo

    Molidustat (BAY 85-3934) , 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 (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.
    Clinical Trial
    Molecular Weight

    314.30

    Formula

    C13H14N8O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1C(N2N=NC=C2)=CNN1C3=NC=NC(N4CCOCC4)=C3
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 5 mg/mL (15.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1817 mL 15.9084 mL 31.8167 mL
    5 mM 0.6363 mL 3.1817 mL 6.3633 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 0.5 mg/mL (1.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 0.5 mg/mL (1.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (31.82 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.70%

    SDS (419 KB)

    COA (249 KB) HNMR (248 KB) RP-HPLC (244 KB) MS (71 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    Rats: BAY 85-3934 is prepared as a solution in ethanol:Solutol HS 15:water (10:20:70). In a repeat-dose, 26-day experiment, male Wistar rats (240–340 g in body weight) are administered vehicle or BAY 85-3934 at doses of 0.5 mg/kg, 1.25 mg/kg, 2.5 mg/kg, and 5 mg/kg. The efficacy of BAY 85-3934 (2.5 mg/kg, once-daily, oral) is also compared with that of rhEPO (25 IU/kg, 50 IU/kg, and 100 IU/kg, twice-weekly, s.c. injection). The time-course of induction of EPO mRNA expression and plasma EPO is determined at baseline and 0.5 h, 1 h, 2 h, 4 h, 6 h, and 8 h after oral administration of a single dose of BAY 85-3934 (5 mg/kg)[1].

    Monkey: BAY 85-3934 is prepared as a solution in 0.5% tylose. Male and female cynomolgus monkeys (2.8–5.6 kg in body weight) are administered at doses of 0.5 mg/kg and 1.5 mg/kg at 0 h, 24 h, 48 h, 72 h, and 96 h. Blood samples are taken at 7 h, 31 h, 55 h, 79 h, 103 h, and 168 h. Erythropoietic parameters are also evaluated after a 2-week treatment period with s.c. administration of rhEPO (100 IU/kg twice weekly at days 1, 4, 8, and 11) and BAY 85-3934 (1.5 mg/kg) once daily[1].

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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.1817 mL 15.9084 mL 31.8167 mL 79.5418 mL
    5 mM 0.6363 mL 3.1817 mL 6.3633 mL 15.9084 mL
    10 mM 0.3182 mL 1.5908 mL 3.1817 mL 7.9542 mL
    15 mM 0.2121 mL 1.0606 mL 2.1211 mL 5.3028 mL
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    Molidustat Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    Molidustat1154028-82-6BAY 85-3934HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHrenal anemiaerythropoietin (EPO)HeLaWistar ratscynomolgus monkeyschronic kidney disease (CKD)Inhibitorinhibitorinhibit

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