Roxadustat (FG-4592)

Catalog No.S1007 Batch:S100706

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Technical Data

Formula

C19H16N2O5
Molecular Weight 352.34 CAS No. 808118-40-3
Solubility (25°C)* In vitro DMSO 70 mg/mL (198.67 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 2.000mg/ml (5.68mM) Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Roxadustat potentiates RSL3 induced ferroptosis. Phase 3.
In vitro

FG-4592 is an oral inhibitor of hypoxia inducible factor (HIF) prolyl hydroxylase currently in clinical development for the treatment of anemia. FG-4592 stabilizes the activities of HIF, a cytosolic transcription factor, leading to activation of the genes associated with erythropoiesis, including erythropoietin and enzymes involved in iron metabolism. [1]
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]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    PC12 cells

  • Concentrations

    50 μM

  • Incubation Time

    6 h

  • Method

    Cell cultures were pre-treated with FG-4592 alone or in the presence of YC-1 for 6 h and then the culture medium was replaced immediately by fresh medium with 150 mM TBHP.
Animal Study:

[2]
  • Animal Models

    Female C57BL/6 mice

  • Dosages

    50 mg/kg

  • Administration

    i.p.

References

  • http://worldwide.espacenet.com/publicationDetails/description?CC=US&NR=2007292433A1&KC=A1&FT=D&ND=3&
  • https://pubmed.ncbi.nlm.nih.gov/26707978/

Customer Product Validation

Immunoblots showing dose-dependent HIF-1α stabilization in U2OS, HeLa and Hep3b (and HIF-2α) cells after 6 hours treatment with FG-4592.

Data from [ , , Chem Sci, 2017, doi: 10.1039/C7SC02103H ]

(A) The viability of the EpSCs in each group was detected by CCK-8 assays. The EpSCs were under the indicated conditions for 24 h. The viability of each group is shown as the mean±SD. *, P<0.05 versus the normoxia control group; #, P<0.05 versus the hypoxia control group. (B) Western blotting results showing that FG-4592 simulated hypoxia-induced increases in HIF-1α and PCNA expression.

Data from [ , , Cell Physiol Biochem, 2018, 46(6):2460-2470 ]

Blood urea nitrogen (A), serum creatinine (B) and serum cystatin C (C) levels. Data were presented as means ± SD (n = 8 in each group). (D) Representative images of periodic acid-Schiff staining (upper: ×100, lower: ×400) of kidneys. (E) Tubular injury score in mice. Data were presented asmeans ± SD of 10 random fields from each kidney (n = 8 in each group).

Data from [ , , Clin Sci, 2018, 132(7):825-838 ]

(B and C) Luciferase reporter activity following treatment with CP-312 or known HIF inducers, FG-4592 and BAY 85-3934, in (B) HIF-1 MIA PaCa-2 and (C) HIF-2-specific PANC-1 luciferase reporter cell lines.

Data from [ , , J Pharmacol Exp Ther, 2018, 364(1):87-96 ]

Selleck's Roxadustat (FG-4592) has been cited by 121 publications

Immunothrombolytic monocyte-neutrophil axes dominate the single-cell landscape of human thrombosis and correlate with thrombus resolution [ Immunity, 2025, S1074-7613(25)00139-6] PubMed: 40280129
HIF-independent oxygen sensing via KDM6A regulates ferroptosis [ Mol Cell, 2025, 85(15):2973-2987.e6] PubMed: 40712585
In Vitro and Ex Vivo Evidences that Pharmacological Induction of the Hypoxia Response Pathway Efficiently Restricts Measles and Nipah Virus Infections [ Emerg Microbes Infect, 2025, 2563067] PubMed: 40958637
Roxadustat regulates the cell cycle and inhibits proliferation of mesangial cells via the hypoxia-inducible factor-1α/P53/P21 pathway [ Front Cell Dev Biol, 2025, 13:1503477] PubMed: 40040789
Cystic fibrosis airway epithelial cells have an exaggerated response to hypoxia that is partially reversible through transmembrane receptor modulation [ J Cyst Fibros, 2025, S1569-1993(25)01561-9] PubMed: 40816946
CRISPR-Cas9 genetic screens reveal regulation of TMPRSS2 by the Elongin BC-VHL complex [ Sci Rep, 2025, 15(1):11907] PubMed: 40195420
Roxadustat alleviates cisplatin-induced acute kidney injury by regulating fatty acid oxidation and mitochondrial function [ Ren Fail, 2025, 47(1):2561218] PubMed: 40968500
Inherent single-cell heterogeneity of the transcriptional response to hypoxia in cancer cells [ NAR Cancer, 2025, 7(3):zcaf021] PubMed: 40918648
Oxygen enhances antiviral innate immunity through maintenance of EGLN1-catalyzed proline hydroxylation of IRF3 [ Nat Commun, 2024, 15(1):3533] PubMed: 38670937
Activation of the hypoxia-inducible factor pathway protects against acute ischemic stroke by reprogramming central carbon metabolism [ Theranostics, 2024, 14(7):2856-2880] PubMed: 38773968

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.