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Roxadustat

🥰Excellent
Catalog No. T2515Cas No. 808118-40-3
Alias FG-4592, ASP1517

Roxadustat (FG-4592) is an orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), with potential anti-anemic activity.

Roxadustat

Roxadustat

🥰Excellent
Purity: 99.94%
Catalog No. T2515Alias FG-4592, ASP1517Cas No. 808118-40-3
Roxadustat (FG-4592) is an orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), with potential anti-anemic activity.
Pack SizePriceAvailabilityQuantity
5 mg$30In Stock
10 mg$48In Stock
25 mg$67In Stock
50 mg$88In Stock
100 mg$118In Stock
500 mg$287In Stock
1 mL x 10 mM (in DMSO)$45In Stock
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Purity:99.94%
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Product Introduction

Bioactivity
Description
Roxadustat (FG-4592) is an orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), with potential anti-anemic activity.
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].
Kinase Assay
Kinase assays: Potencies (IC50 values) are determined by assays of active kinase domains cloned and expressed in baculovirus using the FastBacbaculovirus expression system or obtained commercially. For tyrosine kinase assays, a biotinylated peptide substrate containing a single tyrosine is used with 1 mM ATP, anEu-cryptate–labeled anti-phosphotyrosine antibody (PT66), and Strepavidin-APC in a homogeneous time-resolved fluorescence assay. Serine/threonine kinases are assayed using 5 μM ATP, [33P]ATP, and a biotinylated peptide substrate with peptide capture and incorporation of 33P determined using a SA-Flashplate. Linifanib is assayed at multiple concentrations prepared by serial dilution of a DMSO stock solution of Linifanib. The concentration resulting in 50% inhibition of activity is calculated using nonlinear regression analysis of the concentration response data.
Cell Research
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.
AliasFG-4592, ASP1517
Chemical Properties
Molecular Weight352.34
FormulaC19H16N2O5
Cas No.808118-40-3
SmilesCc1nc(C(=O)NCC(O)=O)c(O)c2ccc(Oc3ccccc3)cc12
Relative Density.1.389 g/cm3
Storage & Solubility Information
Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 60 mg/mL (170.29 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.8382 mL14.1908 mL28.3817 mL141.9084 mL
5 mM0.5676 mL2.8382 mL5.6763 mL28.3817 mL
10 mM0.2838 mL1.4191 mL2.8382 mL14.1908 mL
20 mM0.1419 mL0.7095 mL1.4191 mL7.0954 mL
50 mM0.0568 mL0.2838 mL0.5676 mL2.8382 mL
100 mM0.0284 mL0.1419 mL0.2838 mL1.4191 mL

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