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FG-4592 (Roxadustat; ASP1517) is a novel Hypoxia Inducible Factor Prolyl Hydroxylase inhibitor, in CKD Anemia. FG-4592 is an oral inhibitor of hypoxia inducible factor (HIF) prolyl hydroxylase in clinical development for the treatment of anemia. Stabilization of HIF, a cytosolic transcription factor, by FG-4592 leads to activation of the genes associated with erythropoiesis, including EPO and enzymes involved in iron metabolism.
Biochim Biophys Acta Mol Basis Dis. 2024 Jun 22.
HIF-1 induced tiRNA-Lys-CTT-003 is protective against cisplatin induced ferroptosis of renal tubular cells in mouse AKI model
FG-4592 (Roxadustat) purchased from AbMole
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Source | Hypoxia (2015). Figure 4. FG-4592 |
| Method | oral gavage | |
| Cell Lines | FVB mice | |
| Concentrations | 40 and 80 mg/kg | |
| Incubation Time | 104, 99.5, and 102 days | |
| Results | At this time-point, roxadustat induced a substantial increase in circulating EPO protein (33×), whereas VEGF levels appeared unaffected by treatment. |
| Cell Experiment | |
|---|---|
| Cell lines | PC12 cells |
| Preparation method | Cell viability assay Cell viability was assayed using the Cell Counting Kit-8 (AbMole, M4839) according to the manufacture's protocol. Briefly, PC12 Cells were planted in 96-well plates at a density of 5000 cells per cm2 and incubated at 37 ℃ in a 5% CO2 humidified atmosphere for 24 h. Then the cells were treated with TBHP, FG-4592 and YC-1 as described above. After treatment the cells were washed with PBS, then 100 μL of DMEM and 10 μL of CCK-8 solution was added to each well of 96-well plates, and the plates was incubated for an additional 1 h. The absorbance was then measured at the wavelength of 450 nm by a microplate reader to assess the number of viable cells. |
| Concentrations | 0,5,20,50µM |
| Incubation time | 1h |
| Animal Experiment | |
|---|---|
| Animal models | SCI recovery mice model |
| Formulation | 100 mg FG-4592 was dissolved to 9.675 mL of 5% Dextrose and 325 mL of 1 N NaOH |
| Dosages | 50 mg/kg/day |
| Administration | intraperitoneally |
| Molecular Weight | 352.34 |
| Formula | C19H16N2O5 |
| CAS Number | 808118-40-3 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HIF Products |
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| 2-Methoxyestradiol
2-methoxyestradiol (2-ME2), an endogenous metabolite of 17β -estradiol (E2) with oral activity, is an apoptosis inducer and angiogenesis inhibitor with effective antitumor activity. Methoxyestradiol can also destabilize microtubules. Methoxyestradiol is a potent inhibitor of superoxide dismutase (SOD) and reactive oxygen species (ROS) that can induce autophagy in transformed cell line HEK293, cancer cell line U87 and HeLa. |
| DMOG
DMOG (Dimethyloxaloyl glycine) is an antagonist of α-ketoglutarate cofactor and a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy. |
| IOX2
IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. |
| Hydralazine hydrochloride
Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM. |
| Paeoniflorin
Paeoniflorin is a glycoside isolated from the root of Paeonia lactiflora. Paeoniflorin has been used as an anticonvulsant and has hypoglycemic effect. |
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