Topiroxostat

黄嘌呤氧化还原酶抑制剂(IC50=5.3nM)；抑制分离的人血浆中的ABCG2(IC50=0.18µM)；在5µM浓度下，可增加LPS诱导的Bcl-2水平下降，并降低LPS诱导的Bax和裂解caspase-3水平上升；长期给药会导致尿液中出现黄嘌呤晶体，并在0.2和1mg/kg剂量下诱发大鼠肾病。An inhibitor of xanthine oxidoreductase (IC50 = 5.3 nM); inhibits ABCG2 in isolated human plasma (IC50 = 0.18 µM); increases LPS-induced decreases in Bcl-2 levels and decreases LPS-induced increases of Bax and cleaved caspase-3 levels in H9c2 rat cardiomyocytes at 5 µM; chronic administration results in the presence of urinary xanthine crystals and induces nephropathy in rats at 0.2 and 1 mg/kg, respectively.