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Febuxostat

CAS No. : 144060-53-7

MCE 国际站：Febuxostat

产品活性：Febuxostat (TEI 6720) 是一种有效的、选择性的、非嘌呤 黄嘌呤氧化酶 (XO) 抑制剂，K_i 值为 0.6 nM。Febuxostat 具有研究高尿酸血症和痛风的潜力。

研究领域：Metabolic Enzyme/Protease

作用靶点：Xanthine Oxidase

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.

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.
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.
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.
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.
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.

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