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.
Cell Experiment | |
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Cell lines | PC12 cells |
Preparation method | Cell viability assay Cell viability was assayed using the Cell Counting Kit-8 (CCK-8; Dojindo Co., Kumamoto, Japan) 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 | |
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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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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3-Aminobenzoic acid
3-Aminobenzoic acid is a hypoxia-inducible factor-1α (HIF-1α) inhibitor. |
Steppogenin
Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. |
HIV-IN-7
Axl-IN-16 is a Axl inhibitor. |
HIF-2α-IN-9
HIF-2α-IN-9 is an inhibitor ofHIF-2α. |
PHD-IN-2
PHD-IN-2 is a PHD antagonist (IC50: < 5 nM). |
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