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Febuxostat (TEI-6720) is a non-purine selective xanthine oxidase inhibitor with IC50 of 114 -210 nM. It works by non-competitively blocking the molybdenum pterin center which is the active site on xanthine oxidase. Xanthine oxidase is needed to successively oxidize both hypoxanthine and xanthine to uric acid. Hence, febuxostat inhibits xanthine oxidase, therefore reducing production of uric acid. Febuxostat inhibits both, oxidized as well as reduced form of xanthine oxidase because of which febuxostat cannot be easily displaced from the molybdenum pterin site.
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Source | J Transl Med (2015). Figure 2. Febuxostat |
| Method | apoptosis assay | |
| Cell Lines | H/R and H/R + Veh cells | |
| Concentrations | 1 and 10 μM | |
| Incubation Time | 24 h | |
| Results | 24 h In comparison with Sham group, I/R treatment increased the apoptotic index (34.9 ± 2.6 vs. 4.5 ± 0.9%, P < 0.01). Pretreatment with either febuxostat or allopurinol effectively attenuated the increase in apoptotic index (Febuxostat: 26.9 ± 3.7 vs. 34.9 ± 2.6%; Allopurinol: 29.4 ± 1.9 vs. 34.9 ± 2.6%, P < 0.01, respectively). |
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Source | J Transl Med (2015). Figure 1. Febuxostat |
| Method | Experimental in vivo | |
| Cell Lines | Male C57BL/6 mice | |
| Concentrations | 5 mg/kg | |
| Incubation Time | 24 h | |
| Results | Febuxostat treatment effectively blocked the increase of CK and LDH activities compared with I/R mice (CK: 121.9 ± 16.6 vs. 196.3 ± 15.3 mU/ml; LDH 765.5 ± 166.1 vs. 1549.8 ± 365.8 mU/ml; P < 0.01, respectively), similar to allopurinol (CK: 138.2 ± 7.18 vs. 196.3 ± 15.3 mU/ml; LDH: 1005.9 ± 53.1 vs. 1549.8 ± 365.8 mU/ml; P < 0.01, respectively). |
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Adult male albino Wistar rats |
| Formulation | saline |
| Dosages | 10 mg/kg/day |
| Administration | oral |
| Molecular Weight | 316.37 |
| Formula | C16H16N2O3S |
| CAS Number | 144060-53-7 |
| Form | Solid |
| Solubility (25°C) | DMSO 45 mg/mL |
| Storage | 2-8°C |
| Related Xanthine Oxidase Products |
|---|
| Topiroxostat
Topiroxostat (FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM. |
| Broussoflavonol F
Broussoflavonol F has xanthine oxidase inhibitory activity. |
| Vanillic acid
Vanillic acid inhibits NF-κB activation. Vanillic acid has anti-inflammatory, antibacterial, and chemopreventive effects. |
| 8-Azaadenine
8-Azaadenine |
| Purpurogallin
Purpurogallin is a naturally phenol extracted from the plants of Quercus spp, has potent xanthine oxidase (XO) inhibitory activity with an IC50 of 0.2 µM. Purpurogallin has antioxidant and anti-inflammatory effects. |
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