Febuxostat

强效的黄嘌呤氧化酶抑制剂；抑制牛乳黄嘌呤氧化酶以及小鼠和大鼠肝黄嘌呤氧化酶/黄嘌呤脱氢酶（IC50分别为1.4、1.8和2.2nM）；降低高尿酸血症钾氧杂磷大鼠模型中的血清尿酸水平（ED50=1.5mg/kg）；减少以每天1mg/kg的剂量喂食含有反式脂肪酸的高脂饮食的小鼠的肝脏大泡性脂肪变性；增加GOT2的中枢神经系统表达并改善继发性进行性EAE小鼠模型中的神经系统症状。A potent inhibitor of xanthine oxidase; inhibits bovine milk xanthine oxidase as well as mouse and rat liver xanthine oxidase/xanthine dehydrogenase (IC50s = 1.4, 1.8, and 2.2 nM, respectively); decreases serum urate levels in a potassium oxonate rat model of hyperuricemia (ED50 = 1.5 mg/kg); reduces hepatic macrovesicular steatosis in mice fed a high-fat diet containing trans fatty acids at 1 mg/kg per day; increases CNS expression of GOT2 and improves neurological symptoms in a mouse model of secondary progressive EAE.