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    Roxadustat (FG-4592)
    Roxadustat (FG-4592)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0293
    CAS #: 808118-40-3 Purity ≥98%

    Description: FG-4592 (also known as ASP1517 and Roxadustat) is a novel, orally bioavailable and potent small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH), an enzyme up-regulating the expression of endogenous human erythropoietin (Epo). Roxadustat induces EPO production and stimulates erythropoiesis. It is currently being investigated as an oral treatment for anemia associated with chronic kidney disease (CKD). Unlike other anemia treating agents, erythropoiesis-stimulating agents (ESAs), FG-4592 inhibits HIF, through a distinctive mechanism, by stabilization of HIF. 

    References:Nephrol Dial Transplant. 2015 Oct;30(10):1665-73; Stem Cells Transl Med. 2014 Feb;3(2):135-40.

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    Molecular Weight (MW)

    352.34

    Formula

    C19H16N2O5

    CAS No.

    808118-40-3

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 70 mg/mL (198.7 mM)

    Water: <1 mg/mL

    Ethanol: <1 mg/mL

    Solubility (In vivo)

    5% DMSO+50% PEG 300+ddH2O: 11mg/mL

    Synonyms

    Roxadustat; ASP1517; ASP 1517; ASP-1517; FG-4592; FG 4592; FG4592

    Chemical Name: (4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)glycine

    InChi Key: YOZBGTLTNGAVFU-UHFFFAOYSA-N

    InChi Code: InChI=1S/C19H16N2O5/c1-11-15-9-13(26-12-5-3-2-4-6-12)7-8-14(15)18(24)17(21-11)19(25)20-10-16(22)23/h2-9,24H,10H2,1H3,(H,20,25)(H,22,23)

    SMILES Code: O=C(O)CNC(C1=C(O)C2=C(C(C)=N1)C=C(OC3=CC=CC=C3)C=C2)=O



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    In Vitro

    In vitro activity: 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.

     

    Kinase Assay: FG-4592 (also known as ASP1517 and Roxadustat) is a novel, oral and potent small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH), an enzyme up-regulating the expression of endogenous human erythropoietin (Epo). Roxadustat induces EPO production and stimulates erythropoiesis.

     

    Cell Assay: FG-4592 showed significant protection effect against the TBHP-induced cell death. Cell line used: PC-12 cells. The left eye of each rat is retro-orbitally injected with 25 mg/kg FG-4592 every 2 days, and an equal volume of 20% DMSO diluted with 0.9% NaCl is administrated with retro-orbital injection and served as the control. The retinae (attached, 1 day, 3 days, 5 days, and 7 days after RD) are homogenized and lysed with buffer containing 50 mM hydroxymethyl(Tris)-aminomethane(HCl), 150 mM NaCl, 1% Triton X-100, 1% sodium deoxycholate, 0.1% SDS, and a protease inhibitor tablet. Samples are run on 8% to 12% 2-hydroxyethyl (Bis)-hydroxymethyl (Tris) gel electrophoresis and transferred onto polyvinylidene difluoride (PVDF) membranes (0.2-mm pores). After blocking with 3% nonfat dried milk, the membranes are incubated overnight with primary antibody HIF-1α, LC3, BNIP3, autophagy-related gene 5 (Atg5), and β-actin. The blotted membranes are then incubated for 60 minutes at room temperature with a horseradish peroxidase (HRP)-labeled secondary antibody. Immunoreactive bands are visualized by enhanced chemiluminescence (ECL) and detected with an Amersham Imager 600. A minimum of three rats are used for each condition.

    In Vivo

    In a mouse model of spinal cord injury, FG-4592 administration improved recovery and increased the survival of neurons in spinal cord lesions

    Animal model

    Mouse model of spinal cord injury

    Formulation & Dosage

    50mg/kg/day; i.p.; for 7 days

    References

    Brain Res. 2016 Feb 1;1632:19-26;


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Roxadustat (FG-4592)

    Mean change from BL in Hb (ΔHb) in TIW cohorts (EE population). Nephrol Dial Transplant. 2015 Oct;30(10):1665-73.

    Roxadustat (FG-4592)

    Changes in median plasma EPO on first and final days of treatment. Data are for the PK/PD population (subjects with complete dataset only). Nephrol Dial Transplant. 2015 Oct;30(10):1665-73.

    Roxadustat (FG-4592)

    Mean change from BL in serum hepcidin (EE population). Nephrol Dial Transplant. 2015 Oct;30(10):1665-73.


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