Roxadustat (FG-4592)

Alias: Roxadustat; ASP1517; ASP 1517; ASP-1517; FG-4592; FG4592; FG-4592;
Cat No.:V0293 Purity: ≥98%
Roxadustat (FG4592, ASP1517) is a novel, potent and orally bioavailable inhibitor of HIF-PH (hypoxia-inducible factor prolyl hydroxylase) with the potential to treat anemia associated with chronic kidney disease (CKD).
Roxadustat (FG-4592) Chemical Structure CAS No.: 808118-40-3
Product category: HIF
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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25mg
50mg
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Other Forms of Roxadustat (FG-4592):

  • Roxadustat-d5
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Purity: ≥98%

Product Description

Roxadustat (FG4592, ASP1517) is a novel, potent and orally bioavailable inhibitor of HIF-PH (hypoxia-inducible factor prolyl hydroxylase) with the potential to treat anemia associated with chronic kidney disease (CKD). HIF-PH is an enzyme that can up-regulate the expression of endogenous human erythropoietin (Epo). Roxadustat induces EPO production and stimulates erythropoiesis. It is currently being investigated as an oral treatment for anemia associated with CKD.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In PC12 cells, roxadustat (5-50 μM; 6 hours) dramatically reduces TBHP-induced apoptosis[2]. In PC12 cells, roxadustat (50 μM; 6 hours) stabilizes HIF-1α protein expression[2].
ln Vivo
Improved recovery from spinal cord injury and protection of motor neuron survival are two benefits of roxadustat (50 mg/kg; ip; daily for 7 days)[2].
Cell Assay
Apoptosis Analysis[2]
Cell Types: PC12 cells
Tested Concentrations: 5, 20, 50 μM
Incubation Duration: 6 hrs (hours)
Experimental Results: Dramatically inhibited TBHP-induced apoptosis.

Western Blot Analysis[2]
Cell Types: PC12 cells
Tested Concentrations: 50 μM
Incubation Duration: 6 hrs (hours)
Experimental Results: stabilized HIF-1α protein expression.
Animal Protocol
Animal/Disease Models: 12-week female C57BL/6 mice[2]
Doses: 50 mg/ kg
Route of Administration: intraperitoneal (ip)injection; daily for 7 days
Experimental Results: Protected the survival of motor neurons and improved recovery from spinal cord injury.
References
[1]. Provenzano R, et al. Roxadustat (FG-4592) Versus Epoetin Alfa for Anemia in Patients Receiving MaintenanceHemodialysis: A Phase 2, Randomized, 6- to 19-Week, Open-Label, Active-Comparator, Dose-Ranging, Safety and Exploratory Efficacy Study. Am J Kidney Dis. 2016 Jun;67(6):912-24.
[2]. Wu K, et al. Stabilization of HIF-1α by FG-4592 promotes functional recovery and neural protection in experimental spinal cord injury. Brain Res. 2016 Feb 1;1632:19-26.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H16N2O5
Molecular Weight
352.34100
CAS #
808118-40-3
SMILES
O=C(O)CNC(C1=C(O)C2=C(C(C)=N1)C=C(OC3=CC=CC=C3)C=C2)=O
InChi Key
YOZBGTLTNGAVFU-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H16N2O5/c1-11-15-9-13(26-12-5-3-2-4-6-12)7-8-14(15)18(24)17(21-11)19(25)20-10-16(22)23/h2-9,24H,10H2,1H3,(H,20,25)(H,22,23)
Chemical Name
(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)glycine
Synonyms
Roxadustat; ASP1517; ASP 1517; ASP-1517; FG-4592; FG4592; FG-4592;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 100 mg/mL (~283.82 mM)
H2O : < 0.1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8382 mL 14.1908 mL 28.3817 mL
5 mM 0.5676 mL 2.8382 mL 5.6763 mL
10 mM 0.2838 mL 1.4191 mL 2.8382 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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