Home Angiogenesis HIF modulator - Ferroptosis activator Roxadustat (FG-4592) For research use only.

Roxadustat (FG-4592)

Synonyms: ASP1517

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.

Roxadustat (FG-4592) Chemical Structure

Roxadustat (FG-4592) Chemical Structure

CAS No. 808118-40-3

Purity & Quality Control

Roxadustat (FG-4592) Related Products

Signaling Pathway

HIF Signaling Pathways

HIF Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EpSC cell Cell viability assay 5 µM or 10 µM 24 h FG-4592 increased EpSC cell viability in normoxia. 29742498
Adiposederived mesenchymal stem cells (ADMSCs) Function assay 5 μM the level of HIF-1a expression was much higher in the FG-4592-treated group than in the vehicletreated group. 27021233
Hep3B Function assay 50 to 250 uM 10 hrs Inhibition of HIF-PHD2 in human Hep3B cells assessed as HIF-1alpha protein stabilization at 50 to 250 uM after 10 hrs by Western blot method 29856623
Hep3B Function assay 50 to 250 uM 10 hrs Inhibition of HIF-PHD2 in human Hep3B cells assessed as HIF-2alpha protein stabilization at 50 to 250 uM after 10 hrs by Western blot method 29856623
Hep3B Function assay 50 uM 10 hrs Inhibition of HIF-PHD2 in human Hep3B cells assessed as upregulation of EPO mRNA level at 50 uM after 10 hrs by RT-PCR method 29856623
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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
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]
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot HIF-α CA9 / NDRG1 / GLUT1 / GLUT3 / HK2 / PHD2 / JMJD1A / JMJD2B / JMJD2C 30334352
In Vivo
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]
Animal Research Animal Models Female C57BL/6 mice
Dosages 50 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03303066 Completed
Anemia|Myelodysplastic Syndrome
FibroGen|AstraZeneca
 June 6 2018 Phase 2|Phase 3
NCT02988973 Completed
Chronic Kidney Disease
Astellas Pharma Inc|FibroGen
 January 12 2017 Phase 3
NCT02964936 Completed
Chronic Kidney Disease
Astellas Pharma Inc|FibroGen
 January 11 2017 Phase 3
NCT02952040 Completed
Healthy Subjects
Astellas Pharma Inc|FibroGen
 November 2016 Phase 1
NCT02952092 Completed
Hemodialysis Chronic Kidney Disease Patients With Anemia
Astellas Pharma Inc|FibroGen
 November 30 2016 Phase 3
NCT02805374 Completed
Healthy Subjects
Astellas Pharma Inc|FibroGen
 July 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 352.34 Formula

C19H16N2O5
CAS No. 808118-40-3 SDF Download Roxadustat (FG-4592) SDF
Smiles CC1=C2C=C(C=CC2=C(C(=N1)C(=O)NCC(=O)O)O)OC3=CC=CC=C3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 70 mg/mL ( (198.67 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Can you tell me what the half-life of the product is, please?

Answer:
The half-life of S1007 Roxadustat is around 12 hours. Please the reference below: https://www.ncbi.nlm.nih.gov/pubmed/26846333

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