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

FG-4592 (Synonyms: Roxadustat)

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

FG-4592 is an oral hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor, currently used for the treatment of anemia.

For research use only. We do not sell to patients.
FG-4592 Chemical Structure

FG-4592 Chemical Structure

CAS No. : 808118-40-3

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $66 In-stock
10 mg $60 In-stock
50 mg $200 In-stock
100 mg $320 In-stock
200 mg $400 In-stock
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Customer Review

    FG-4592 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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    FG-4592 is an oral hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor, currently used for the treatment of anemia.

    In Vitro

    FG-4592 significantly increases accumulation of HIF-1α and BNIP3, resultes in reduced TUNEL-positive photoreceptors 3 days after RD and an increased thickness of the outer nuclear layer 7 days after RD in the TUNEL-positive cells[1]. FG-4592 increases differentiation of adipose-derived mesenchymal stem cells (ADMSCs) under both hypoxia and normoxia[2].

    In Vivo

    FG-4592 (25 mg/kg) enhances mitophagy and attenuates retinal histopathologic damage in the photoreceptor layer after RD in an RD animal model[1].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT01630889 FibroGen Chronic Kidney Disease|End Stage Renal Disease|Anemia May 2012 Phase 2|Phase 3
    NCT02161224 Astellas Pharma Europe B.V.|FibroGen|Astellas Pharma Inc PK of FG-4592|Hepatic Insufficiency|Healthy Subjects September 2013 Phase 1
    NCT02161796 Astellas Pharma Europe B.V.|FibroGen|Astellas Pharma Inc PK for FG-4592|Healthy Subjects September 2013 Phase 1
    NCT02252731 Astellas Pharma Europe B.V.|FibroGen|Astellas Pharma Inc Pharmacokinetics of FG-4592|Healthy Subjects September 2013 Phase 1
    NCT01376063 FibroGen Healthy Adult Subjects March 2010 Phase 1
    NCT01750190 FibroGen|Astellas Pharma Europe B.V.|AstraZeneca CKD Anemia November 2012 Phase 3
    NCT01596855 FibroGen|Ruijin Hospital|RenJi Hospital|Chang Zheng Hospital|Xinhua Hospital, Shanghai Jiao Tong University School of Medicine|Peking University First Hospital|First Affiliated Hospital, Sun Yat-Sen University|First Affiliated Hospital of Zhejiang University|Peking Union Medical College Hospital|Shenzhen People's Hospital Anemia in End Stage Renal Disease September 2011 Phase 2
    NCT00761657 FibroGen Chronic Kidney Disease|Anemia November 2008 Phase 2
    NCT01244763 FibroGen Chronic Kidney Disease|Anemia October 2010 Phase 2
    NCT02652806 FibroGen Anemia December 2015 Phase 3
    NCT02652819 FibroGen Anemia December 2015 Phase 3
    NCT01599507 FibroGen Anemia in Chronic Kidney Disease December 2011 Phase 2
    NCT02052310 FibroGen|Astellas Pharma Europe B.V.|AstraZeneca Anemia in Incident Dialysis Patients December 2013 Phase 3
    NCT01414075 FibroGen Dialysis|Anemia July 2011 Phase 2
    NCT01147666 FibroGen End Stage Renal Disease|Anemia March 2010 Phase 2
    NCT02273726 FibroGen|Astellas Pharma Europe B.V.|AstraZeneca CKD Anemia in Stable Dialysis Patients December 2014 Phase 3
    NCT02021318 Astellas Pharma Europe B.V.|FibroGen|Astellas Pharma Inc Anemia in Chronic Kidney Disease in Non-dialysis Patients February 2014 Phase 3
    NCT02965040 Astellas Pharma Europe B.V.|FibroGen|Astellas Pharma Inc Normal Renal Function|Impaired Renal Function December 12, 2016 Phase 1
    NCT02174731 AstraZeneca|FibroGen Anemia July 1, 2014 Phase 3
    NCT01887600 Astellas Pharma Europe B.V.|FibroGen|Astellas Pharma Inc Anemia in Chronic Kidney Disease in Non-dialysis Patients September 3, 2013 Phase 3
    NCT02174627 AstraZeneca|FibroGen Anemia June 26, 2014 Phase 3
    NCT02278341 Astellas Pharma Europe B.V.|FibroGen|Astellas Pharma Inc Anemia|End Stage Renal Disease (ESRD) November 21, 2014 Phase 3
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) 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
    Cell Assay
    [1]

    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.  MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    The rats are anesthetized with 1% sodium pentobarbital, and the pupils are dilated with 0.5% tropicamide and 0.5% phenylephrine hydrochloride eye drops. In each rat, the sclera is punctured approximately 1.5 mm posterior to the limbus with a 30-gauge needle with special caution taken to avoid damaging the lens. The needle is slowly advanced into the vitreous cavity through the sclerotomy and then to the subretinal space by producing a small hole in the peripheral retina. Sodium hyaluronate (10 mg/mL) is slowly injected until almost two-thirds of the neurosensory retina detached from the underlying RPE. RD is confirmed for each rat by a surgical microscope. The blebs of RD are created and remained essentially stable for 7 days. All of the procedure steps are performed on the left eyes of the control group, except for the introduction of the subretinal injector and injection of the sodium hyaluronate. A total of 102 rats are used, and all animal experiments contained at least three rats per group. FG-4592 is dissolved in 20% dimethyl sulfoxide (DMSO) and diluted with 0.9% sodium chloride (NaCl). 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. All of the detection time points are selected at 4 to 6 hours after retro-orbital injection.   MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    352.34

    Formula

    C₁₉H₁₆N₂O₅

    CAS No.

    808118-40-3

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 46 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.91%

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    FG-4592
    Cat. No.:
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