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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: Roxadustat (FG4592, ASP1517) is a novel, potent and orally bioavailable inhibitor of HIF-PH (hypoxia-inducible factor prolyl hydroxylase) with the potential to treat anemia associated with chronic kidney disease (CKD). HIF-PH is an enzyme that can up-regulate 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 CKD. 

    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; FG4592; FG-4592;

    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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