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

Roxadustat (Synonyms: FG-4592)

Cat. No.: HY-13426 Purity: 99.91%
Handling Instructions

Roxadustat is an oral hypoxia-inducible factor prolyl-hydroxylase 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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
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50 mg USD 108 In-stock
Estimated Time of Arrival: December 31
100 mg USD 144 In-stock
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200 mg USD 228 In-stock
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500 mg USD 348 In-stock
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1 g USD 540 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.

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

    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 MCE. Usage Cited in: J Cell Mol Med. 2019 Jan;23(1):349-356.

    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.
    • Biological Activity

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    • Customer Review

    Description

    Roxadustat is an oral hypoxia-inducible factor prolyl-hydroxylase 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].

    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].

    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.

    808118-40-3

    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)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.2838 mL 1.4191 mL 2.8382 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

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

      Solubility: 2.5 mg/mL (7.10 mM); Precipitated solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.91%

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    Product Name:
    Roxadustat
    Cat. No.:
    HY-13426
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