Roxadustat (FG-4592)

Catalog No.S1007 Batch:S100704

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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
* <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.)

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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.

Customer Product Validation

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

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

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

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

Selleck's Roxadustat (FG-4592) has been cited by 100 publications

Single-embryo transcriptomic atlas of oxygen response reveals the critical role of HIF-1α in prompting embryonic zygotic genome activation [ Redox Biol, 2024, 72:103147] PubMed: 38593632
Factor inhibiting HIF negatively regulates antiviral innate immunity via hydroxylation of IKKϵ [ Cell Rep, 2024, 43(1):113606.] PubMed: 38127621
Inhibition of OGFOD1 by FG4592 confers neuroprotection by activating unfolded protein response and autophagy after ischemic stroke [ J Transl Med, 2024, 22(1):248] PubMed: 38454480
The N6-methyladenosine demethylase ALKBH5 regulates the hypoxic HBV transcriptome [ PLoS Pathog, 2024, 20(1):e1011917] PubMed: 38227578
Mitophagy mediated by HIF-1α/FUNDC1 signaling in tubular cells protects against renal ischemia/reperfusion injury [ Ren Fail, 2024, 46(1):2332492] PubMed: 38584135
Hypoxia-inducible factor upregulation by roxadustat attenuates drug reward by altering brain iron homoeostasis [ Signal Transduct Target Ther, 2023, 10.1038/s41392-023-01578-2] PubMed: 37718358
Hypoxia-inducible factor upregulation by roxadustat attenuates drug reward by altering brain iron homoeostasis [ Signal Transduct Target Ther, 2023, 8(1):355] PubMed: 37718358
Hypoxia stabilizes SETDB1 to maintain genome stability [ Nucleic Acids Res, 2023, gkad796] PubMed: 37850636
Osteocyte Egln1/Phd2 links oxygen sensing and biomineralization via FGF23 [ Bone Res, 2023, 11(1):7] PubMed: 36650133
Selective induction of human renal interstitial progenitor-like cell lineages from iPSCs reveals development of mesangial and EPO-producing cells [ Cell Rep, 2023, S2211-1247(23)01614-5] PubMed: 38237600

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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.