2. Metabolic Enzyme/Protease Apoptosis
  3. HIF/HIF Prolyl-Hydroxylase Ferroptosis
  4. Roxadustat

Roxadustat is an orally active hypoxia-inducible factor (HIF) prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin.

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

Roxadustat Chemical Structure

Roxadustat Chemical Structure

CAS No. : 808118-40-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 38 In-stock
10 mg USD 60 In-stock
50 mg USD 108 In-stock
100 mg USD 144 In-stock
200 mg USD 228 In-stock
500 mg USD 348 In-stock
1 g USD 540 In-stock
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Customer Review

Based on 41 publication(s) in Google Scholar

Other Forms of Roxadustat:

Roxadustat Related Antibodies

Top Publications Citing Use of Products

38 Publications Citing Use of MCE Roxadustat

WB
IF

    Roxadustat purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2019 Jan;23(1):349-356.  [Abstract]

    FG-4592 increases level of HIF-1α and regulates apoptosis-related proteins in AHH-1. The effects of FG-4592 on HIF1-α are detected using Western Blot. Level of HIF-1α is measured at different time points after the treatment of FG-4592 (A). Cell lysate is obtained at 6 h after irradiation and used to evaluate the regulation of FG-4592 on apoptosis-related molecules. Apoptosis promoting molecules (c-caspase3 and cyt-c) are downregulated and molecules that inhibit apoptosis are up-regulated by FG-4

    Roxadustat purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2019 Jan;23(1):349-356.  [Abstract]

    FG-4592 mitigates radiation-induced DNA injuries. AHH-1 cells pretreated with or without FG-4592 are exposed to 6 Gy irradiation and γ-H2AX assay is used to determine DNA damages at 0, 0.5, 2 h after irradiation.

    Roxadustat purchased from MedChemExpress. Usage Cited in: Science. 2016 Apr 1;352(6281):54-61.  [Abstract]

    FG-4592 causes normoxic stabilization of HIF1α and rewires energy metabolism. Immunoblot showing HIF1α ± RC inhibition with antimycin or oligomycin, ± FG-4592 under normoxia (21% O2) or hypoxia (1% O2). RC inhibition prevents HIF1α stabilization during hypoxia. FG-4592 administration overcomes this paradox and stabilizes HIF1α even during normoxia. Immunoblot is representative of independent experiments done in duplicate in HT-29 cells.

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

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    HIF-1α HIF

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Roxadustat is an orally active hypoxia-inducible factor (HIF) prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin[1].

    IC50 & Target

    Hypoxia-inducible factor prolyl-hydroxylase[1]
    In Vitro

    Roxadustat (5-50 μM; 6 hours) significantly inhibits TBHP-induced apoptosis in PC12 cells[2].
    Roxadustat (50 μM; 6 hours) stabilizes HIF-1α protein expression in PC12 cells[2].

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

    Roxadustat Related Antibodies

    Apoptosis Analysis[2]

    Cell Line: PC12 cells
    Concentration: 5, 20, 50 μM
    Incubation Time: 6 hours
    Result: Significantly inhibited TBHP-induced apoptosis.

    Western Blot Analysis[2]

    Cell Line: PC12 cells
    Concentration: 50 μM
    Incubation Time: 6 hours
    Result: stabilized HIF-1α protein expression.
    In Vivo

    Roxadustat (50 mg/kg; i.p.; daily for 7 days) protects the survival of motor neurons and improves recovery from spinal cord injury[2].

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

    Animal Model: 12-week female C57BL/6 mice[2]
    Dosage: 50 mg/kg
    Administration: Intraperitoneal injection; daily for 7 days
    Result: Protected the survival of motor neurons and improved recovery from spinal cord injury.
    Clinical Trial
    Molecular Weight

    352.34

    Formula

    C19H16N2O5
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    O=C(O)CNC(C1=C(O)C2=C(C(C)=N1)C=C(OC3=CC=CC=C3)C=C2)=O
    Shipping

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

    DMSO : 100 mg/mL (283.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8382 mL 14.1908 mL 28.3817 mL
    5 mM 0.5676 mL 2.8382 mL 5.6763 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 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)

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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: ≥ 2.5 mg/mL (7.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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: 5 mg/mL (14.19 mM); Suspended solution; Need ultrasonic

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

    Dosage

    mg/kg

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    Dosing volume
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    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: 99.91%

    COA (245 KB) HNMR (175 KB) LCMS (439 KB)

    Handling Instructions (2659 KB)
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8382 mL 14.1908 mL 28.3817 mL 70.9542 mL
    5 mM 0.5676 mL 2.8382 mL 5.6763 mL 14.1908 mL
    10 mM 0.2838 mL 1.4191 mL 2.8382 mL 7.0954 mL
    15 mM 0.1892 mL 0.9461 mL 1.8921 mL 4.7303 mL
    20 mM 0.1419 mL 0.7095 mL 1.4191 mL 3.5477 mL
    25 mM 0.1135 mL 0.5676 mL 1.1353 mL 2.8382 mL
    30 mM 0.0946 mL 0.4730 mL 0.9461 mL 2.3651 mL
    40 mM 0.0710 mL 0.3548 mL 0.7095 mL 1.7739 mL
    50 mM 0.0568 mL 0.2838 mL 0.5676 mL 1.4191 mL
    60 mM 0.0473 mL 0.2365 mL 0.4730 mL 1.1826 mL
    80 mM 0.0355 mL 0.1774 mL 0.3548 mL 0.8869 mL
    100 mM 0.0284 mL 0.1419 mL 0.2838 mL 0.7095 mL
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    Roxadustat 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:

    Roxadustat808118-40-3FG-4592FG4592FG 4592HIF/HIF Prolyl-HydroxylaseFerroptosisHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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