Roxadustat FG-4592

Roxadustat (FG-4592) Research Standard

Roxadustat (FG-4592, ASP 1517) is a potent, synthetic small-molecule inhibitor of the hypoxia-inducible factor prolyl hydroxylase (HIF-PH) enzymes. Characterized by an isoquinoline carboxamide scaffold, this compound serves as a critical biochemical tool for investigating oxygen-sensing pathways and cellular responses to hypoxia. In laboratory research, it is utilized as a competitive inhibitor to map enzyme-substrate interactions, assess binding affinity through kinetic assays, and probe the biochemical regulation of HIF-alpha subunit stability in isolated enzyme systems.

Technical Specifications

Mechanism of Action & Research Context

Roxadustat functions as a competitive inhibitor of the HIF-prolyl hydroxylase (PH) enzymes, which are responsible for the degradation of Hypoxia-Inducible Factor (HIF) under normoxic conditions.

• Substrate Mimicry: The glycine amide group within the Roxadustat molecule acts as a mimetic of natural substrates, allowing the compound to occupy the enzyme’s active site.

• Active Site Binding: By binding to the site where oxygen and 2-oxoglutarate would normally interact, the molecule prevents the hydroxylation of HIF-alpha subunits.

• Structural Stabilization: The phenoxy acetic acid moiety provides additional stability to the ligand-enzyme complex, allowing for the precise measurement of binding kinetics in cell-free assays.

Research Applications

Roxadustat is a specialized reagent used to investigate the kinetics and regulatory mechanisms of prolyl hydroxylase enzymes.

Primary fields of in vitro laboratory investigation include:

• Enzyme Binding Assays: Measuring the efficacy of HIF-PH inhibition in isolated protein preparations and cell-free assay systems.

• Competition Studies: Observing the displacement of natural substrates by Roxadustat to determine competitive binding characteristics.

• Binding Affinity (Kinetics): Utilizing kinetic methods to establish inhibition constants and understand the stability of the enzyme-inhibitor complex.

• Stability & Degradation Testing: Monitoring the chemical degradation of the compound under diverse environmental and solvent conditions to refine laboratory protocol standards.

Storage & Handling Guidelines

To maintain the chemical stability and experimental reliability of the compound:

• General Storage: Keep the powder and capsules in a sealed, dry container at room temperature.

• Environmental Control: Protect from direct sunlight; store in a dark cabinet or opaque container to preserve molecular integrity.

• Moisture Protection: Store powder with an appropriate desiccant to prevent hydration and ensure the accuracy of weight measurements.

• Container Integrity: Always close the container tightly immediately after each use to minimize atmospheric exposure.

Research Use Disclaimer

Research Use Only Disclaimer: This product is developed and distributed strictly as a Research Use Only (RUO) laboratory reference chemical intended exclusively for non-clinical analytical and scientific investigation. It is not an FDA-approved drug, medical treatment, dietary supplement, or food ingredient, and is strictly prohibited for human or animal consumption. Kimera Chems supplies this high-purity research material solely to qualified institutions and professional investigators for authorized laboratory research.