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 | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| 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 |
| 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.
| Related Xanthine Oxidase Products |
|---|
| H-Tyr-Phe-OH
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. |
| TEI-6469
TEI-6469 is a xanthine oxidase (XO) inhibitor that may be used in studies related to gout. |
| Phytic acid dodecasodium hydrate
Phytic acid (Inositol hexaphosphate) dodecasodium hydrate is a phosphorus storage compound of seeds and cereal grains. |
| Ellagic acid-4-O-beta-D-xylopyranoside
Ellagic acid 4-O-β-D-xylopyranoside is a natural ellagitannin with antimicrobial activity. Ellagic acid 4-O-β-D-xylopyranoside is an xanthine oxidase inhibitor with an 50 of 2.1 μg/mL. |
| Protosappanin A dimethyl acetal
Protosappanin A dimethyl acetal is a homoisoflavonoid. |
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