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Febuxostat

Cat. No. M1711
Febuxostat Structure
Synonym:

Uloric, TMX-67

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM/1mL In DMSO USD 90 In stock
10mg USD 65 In stock
50mg USD 150 In stock
100mg USD 240 In stock
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Quality Control
Biological Activity

Febuxostat (Uloric) 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.

Customer Product Validations & Biological Datas
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).
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).
Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 316.37
Formula C16H16N2O3S
CAS Number 144060-53-7
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

Efficacy and safety of febuxostat in patients with hyperuricemia and gout.
Garcia-Valladares et al. Ther Adv Musculoskelet Dis. 2011 Oct;3(5):245-53. PMID: 22870483.

Cardiovascular safety of febuxostat and allopurinol in patients with gout and cardiovascular comorbidities.
White et al. Am Heart J. 2012 Jul;164(1):14-20.. PMID: 22795277.

Development and validation of a liquid chromatography-tandem mass spectrometry method for the determination of febuxostat in human plasma.
Wang et al. Biomed Chromatogr. 2012 May 24. PMID: 22623034.

Use of newly available febuxostat in a case of chronic tophaceous gout contraindicated to allopurinol and probenecid.
Hilmi et al. Med J Malaysia. 2012 Feb;67(1):125-6. PMID: 22582566.

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Abmole Inhibitor Catalog 2017




Keywords: Febuxostat, Uloric, TMX-67 supplier, OX Receptor, inhibitors

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