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.
|Animal models||Adult male albino Wistar rats|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
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.
|Related OX Receptor Products|
SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).
MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.
SB408124 (Tocris-1963) is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.
Suvorexant (MK-4305) is a potent, selective and orally bioavailable antagonist of OX(1)R and OX(2)R for the treatment of insomnia.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.