CAS NO: | 808118-40-3 |
规格: | ≥98% |
包装 | 价格(元) |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
1g | 电议 |
2g | 电议 |
Molecular Weight (MW) | 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 | Roxadustat; ASP1517; ASP 1517; ASP-1517; FG-4592; FG4592; FG-4592; Chemical Name: (4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)glycine 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) SMILES Code: O=C(O)CNC(C1=C(O)C2=C(C(C)=N1)C=C(OC3=CC=CC=C3)C=C2)=O |
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: FG-4592 (also known as ASP1517 and Roxadustat) is a novel, oral and potent small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH), an enzyme up-regulating the expression of endogenous human erythropoietin (Epo). Roxadustat induces EPO production and stimulates erythropoiesis.
Cell Assay: FG-4592 showed significant protection effect against the TBHP-induced cell death. Cell line used: PC-12 cells. The left eye of each rat is retro-orbitally injected with 25 mg/kg FG-4592 every 2 days, and an equal volume of 20% DMSO diluted with 0.9% NaCl is administrated with retro-orbital injection and served as the control. The retinae (attached, 1 day, 3 days, 5 days, and 7 days after RD) are homogenized and lysed with buffer containing 50 mM hydroxymethyl(Tris)-aminomethane(HCl), 150 mM NaCl, 1% Triton X-100, 1% sodium deoxycholate, 0.1% SDS, and a protease inhibitor tablet. Samples are run on 8% to 12% 2-hydroxyethyl (Bis)-hydroxymethyl (Tris) gel electrophoresis and transferred onto polyvinylidene difluoride (PVDF) membranes (0.2-mm pores). After blocking with 3% nonfat dried milk, the membranes are incubated overnight with primary antibody HIF-1α, LC3, BNIP3, autophagy-related gene 5 (Atg5), and β-actin. The blotted membranes are then incubated for 60 minutes at room temperature with a horseradish peroxidase (HRP)-labeled secondary antibody. Immunoreactive bands are visualized by enhanced chemiluminescence (ECL) and detected with an Amersham Imager 600. A minimum of three rats are used for each condition. |
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; |