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Roxadustat (FG-4592) HIF Proly Hydroxylase inhibitor

Name: Roxadustat (FG-4592)
Brand: Selleck Chemicals
SKU: S1007
Availability: InStock
Rating: 5 (116 reviews)

Cat.No.S1007

Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. This compound also potentiates RSL3 induced ferroptosis. Phase 3.

Chemical Structure

Molecular Weight: 352.34

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.96%

99.96

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	352.34	Formula	C₁₉H₁₆N₂O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	808118-40-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ASP1517			Smiles	CC1=C2C=C(C=CC2=C(C(=N1)C(=O)NCC(=O)O)O)OC3=CC=CC=C3

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (198.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (5.68mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (28.38mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

In vitro	Roxadustat (FG-4592) is an oral inhibitor of hypoxia inducible factor (HIF) prolyl hydroxylase currently in clinical development for the treatment of anemia. It 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 (FG-4592) (50 mg/kg; i.p.; daily for 7 days) protects the survival of motor neurons and improves recovery from spinal cord injury.^[2]
References	[1] http://worldwide.espacenet.com/publicationDetails/description?CC=US&NR=2007292433A1&KC=A1&FT=D&ND=3& [2] https://pubmed.ncbi.nlm.nih.gov/26707978/

Applications

Methods	Biomarkers	Images	PMID
Western blot	HIF-α CA9 / NDRG1 / GLUT1 / GLUT3 / HK2 / PHD2 / JMJD1A / JMJD2B / JMJD2C		30334352

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

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

Answer:
Its half-life is around 12 hours. Please see the reference below: https://www.ncbi.nlm.nih.gov/pubmed/26846333

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