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FG-4592

Cat. No. M1726
FG-4592 Structure
Synonym:

ASP1517

Size Price Availability Quantity
25mg USD 120 In stock
50mg USD 200 In stock
200mg USD 440 In stock
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Quality Control
Biological Activity

FG-4592 (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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 352.34
Formula C19H16N2O5
CAS Number 808118-40-3
Purity 100.00%
Solubility DMSO 70 mg/mL
Storage at -20°C
References

Hypoxia-inducible factor stabilizers and other small-molecule erythropoiesis-stimulating agents in current and preventive doping analysis.
Beuck S, et al. Drug Test Anal. 2012 Nov;4(11):830-45. PMID: 22362605.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: FG-4592, ASP1517 supplier, HIF, inhibitors

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