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Biological Activity for Roxadustat
Roxadustat is a hypoxia-inducible factor prolyl hydroxylase enzyme (HIF-PH) inhibitor (IC50 = 591.4 nM). Roxadustat reduces basal oxygen consumption and increases glycolysis in vitro. It increases hemoglobin levels and stimulates erythropoiesis in vivo. By reducing ACE2 expression, roxadustat reduces the levels of SARS-CoV-2 viral RNA and inhibits entry, replication and secretion of infectious particles in lung epithelial cells. Roxadustat also suppresses hydroxylation and secretion of high molecular weight forms of mannose-binding lectin. The compound suppresses ion currents in pituitary tumor cells (IC50 values for inhibition of peak and late components of delayed rectifier calcium currents are 5.71 and 1.32 μM, respectively). Orally bioavailable.
Technical Data for Roxadustat
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Roxadustat
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Roxadustat
The following data is based on the product molecular weight 352.35. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.84 mL||14.19 mL||28.38 mL|
|5 mM||0.57 mL||2.84 mL||5.68 mL|
|10 mM||0.28 mL||1.42 mL||2.84 mL|
|50 mM||0.06 mL||0.28 mL||0.57 mL|
References for Roxadustat
References are publications that support the biological activity of the product.
Chang et al (2019) Evidence for the capability of roxadustat (FG-4592), an oral HIF prolyl-hydroxylase inhibitor, to perturb membrane ionic currents:an unidentified yet important action. Int.J.Mol.Sci. 20 6027 PMID: 31795416
Wu et al (2018) Click chemistry-based discovery of [3-Hydroxy-5-(1H-1,2,3-triazol-4-yl)picolinoyl]glycines as orally active hypoxia-inducing factor prolyl hydroxylase inhibitors with favorable safety profiles for the treatment of anemia. J.Med.Chem. 61 5332
Jain et al (2016) Hypoxia as a therapy for mitochondrial disease. Science 352 54 PMID: 26917594
Bhute et al (2020) Mannose binding lectin is hydroxylated by collagen prolyl-4-hydroxylase and inhibited by some PHD inhibitors. Kidney360 2
Provenzano et al (2016) Oral hypoxia-inducible factor prolyl hydroxylase inhibitor roxadustat (FG-4592) for the treatment of anemia in patients with CKD. Clin.J.Am.Soc.Nephrol. 11 982 PMID: 27094610
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Keywords: Roxadustat, Roxadustat supplier, FG4592, hypoxia, hydroxylase, inhibitors, erythropoiesis, ion, channels, currents, HIF, hemoglobin, virus, viral, ACE2, FG, 4592, Hydroxylases, Voltage-Gated, Potassium, Channels, 7486, Tocris Bioscience
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