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FG-4592 (Roxadustat)

Cat. No. M1726
FG-4592 (Roxadustat) Structure
Synonym:

Roxadustat; ASP1517

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 50  USD50 In stock
10mg USD 47  USD47 In stock
25mg USD 83  USD83 In stock
50mg USD 155  USD155 In stock
100mg USD 200  USD200 In stock
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Quality Control & Documentation
Biological Activity

FG-4592 (Roxadustat; ASP1517) is a novel Hypoxia Inducible Factor Prolyl Hydroxylase inhibitor, in CKD Anemia. FG-4592 is an oral inhibitor of hypoxia inducible factor (HIF) prolyl hydroxylase in clinical development for the treatment of anemia. Stabilization of HIF, a cytosolic transcription factor, by FG-4592 leads to activation of the genes associated with erythropoiesis, including EPO and enzymes involved in iron metabolism.

Customer Product Validations & Biological Datas
Source Hypoxia (2015). Figure 4. FG-4592
Method oral gavage
Cell Lines FVB mice
Concentrations 40 and 80 mg/kg
Incubation Time 104, 99.5, and 102 days
Results At this time-point, roxadustat induced a substantial increase in circulating EPO protein (33×), whereas VEGF levels appeared unaffected by treatment.
Protocol (for reference only)
Cell Experiment
Cell lines PC12 cells
Preparation method Cell viability assay Cell viability was assayed using the Cell Counting Kit-8 (CCK-8; Dojindo Co., Kumamoto, Japan) according to the manufacture's protocol. Briefly, PC12 Cells were planted in 96-well plates at a density of 5000 cells per cm2 and incubated at 37 ℃ in a 5% CO2 humidified atmosphere for 24 h. Then the cells were treated with TBHP, FG-4592 and YC-1 as described above. After treatment the cells were washed with PBS, then 100 μL of DMEM and 10 μL of CCK-8 solution was added to each well of 96-well plates, and the plates was incubated for an additional 1 h. The absorbance was then measured at the wavelength of 450 nm by a microplate reader to assess the number of viable cells.
Concentrations 0,5,20,50µM
Incubation time 1h
Animal Experiment
Animal models SCI recovery mice model
Formulation 100 mg FG-4592 was dissolved to 9.675 mL of 5% Dextrose and 325 mL of 1 N NaOH
Dosages 50 mg/kg/day
Administration intraperitoneally
Chemical Information
Molecular Weight 352.34
Formula C19H16N2O5
CAS Number 808118-40-3
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Beuck S, et al. Drug Test Anal. Hypoxia-inducible factor stabilizers and other small-molecule erythropoiesis-stimulating agents in current and preventive doping analysis.

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Keywords: FG-4592 (Roxadustat), Roxadustat; ASP1517 supplier, HIF, inhibitors, activators


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