Roxadustat

Name: Roxadustat
Brand: Tocris Bioscience
SKU: 7486

Tocris Bioscience, part of Bio-Techne | Catalog # 7486

COA / SDS

HIF-PH inhibitor; erythropoietic

Key Product Details

Description:	HIF-PH inhibitor; erythropoietic
Alternative Names:	FG 4592
Chemical Name:	N-[(4-Hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]glycine
Purity:	≥98% (HPLC)
Molecular Weight:	352.35

View Full Technical Details for Roxadustat

Technical Data
Citations

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

M. Wt	352.35
Formula	C₁₉H₁₆N₂O₅
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	808118-40-3
PubChem ID	11256664
InChi Key	YOZBGTLTNGAVFU-UHFFFAOYSA-N
Smiles	O=C(O)CNC(=O)C=1N=C(C=2C=C(OC=3C=CC=CC3)C=CC2C1O)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 for Roxadustat

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	35.23	100

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

References for Roxadustat

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