Roxadustat

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Provenzano Oral hypoxia-inducible factor prolyl hydroxylase inhibitor roxadustat (FG-4592) for the treatment of anemia in patients with CKD. Clin.J.Am.Soc.Nephrol. 2016 PMID: 27094610
• Bhute Mannose binding lectin is hydroxylated by collagen prolyl-4-hydroxylase and inhibited by some PHD inhibitors. Kidney360
• Wu 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.
• Jain Hypoxia as a therapy for mitochondrial disease. Science 2016 PMID: 26917594
• Chang 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. 2019 PMID: 31795416