Febuxostat

Febuxostat (TEI 6720) is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a K_i value of 0.6 nM. Febuxostat has the potential for the research of hyperuricemia and gout^[1][2][3]. IC50 & Target:Ki: 0.6 nM (Xanthine oxidase)^[1] In Vitro: Febuxostat displays potent mixed-type inhibition of the activity of purified bovine milk xanthine oxidase, with K_i and K_i' values of 0.6 nM and 3.1 nM respectively, indicating inhibition of both the oxidized and reduced forms of xanthine oxidase^[1]. In Vivo: Febuxostat (5-6 mg/kg; i.e.; daily for 4 weeks) (fed a high-fructose diet (60% fructose) for 8 wk) significantly reduces lomerular pressure, renal vasoconstriction, and afferent arteriolar area relative to fructose+P rats, and shows no significant effects in rats on a normal diet when febuxostat treatment alone^[2].
Febuxostat (3-4 mg/kg; p.o.; daily for 4 weeks) with oxonic acid (750 mg/kg; oral gavage; daily for 4 weeks) preventes renal injury in 5/6 Nx (5/6 nephrectomy) rats with and without coexisting hyperuricemia^[3].
Febuxostat (2.5 mg/kg; p.o.; daily for 12 weeks) inhibits plaque formation in ApoE−/− mice and reduces the levels of ROS in the aortic wall of atherosclerotic mice^[4].
Febuxostat (15.6 mg/kg; p.o.; once daily for 21 successive days) shows antidepressant effect by significantly reduces the immobility time in the FST in mouse^[5].
Febuxostat (10 mg/kg; p.o.; daily for 21 days) administration with doxorubicin caused a significant decrease in nephrotoxicity markers and inflammatory mediators, restoration of normal values of oxidative stress biomarkers and hampering the expression of renal caspase-3^[6].