product name Roxadustat (FG-4592)
Description: FG-4592 (also known as ASP1517) is a potent small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH), an enzyme up-regulating the expression of endogenous human erythropoietin (Epo). It is currently being investigated as an oral treatment for anemia associated with chronic kidney disease (CKD). Unlike other anemia treating agents, erythropoiesis-stimulating agents (ESAs), FG-4592 inhibits HIF, through a distinctive mechanism, by stabilization of HIF.
References: Nephrol Dial Transplant. 2015 Oct;30(10):1665-73; Stem Cells Transl Med. 2014 Feb;3(2):135-40.
352.34
Formula
C19H16N2O5
CAS No.
808118-40-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 70 mg/mL (198.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
5% DMSO+50% PEG 300+ddH2O: 11mg/mL
Synonyms
ASP1517
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19426444
| In Vitro |
In vitro activity: FG-4592 is an oral inhibitor of hypoxia inducible factor (HIF) prolyl hydroxylase currently in clinical development for the treatment of anemia. FG-4592 stabilizes the activities of HIF, a cytosolic transcription factor, leading to activation of the genes associated with erythropoiesis, including erythropoietin and enzymes involved in iron metabolism. Kinase Assay: Cell Assay: FG-4592 showed significant protection effect against the TBHP-induced cell death. Cell line used: PC-12 cells. |
|---|---|
| In Vivo | In a mouse model of spinal cord injury, FG-4592 administration improved recovery and increased the survival of neurons in spinal cord lesions |
| Animal model | Mouse model of spinal cord injury |
| Formulation & Dosage | 50mg/kg/day; i.p.; for 7 days |
| References | Brain Res. 2016 Feb 1;1632:19-26; |
