Febuxostat (TEI 6720) sodium 是一种有效的、选择性的、非嘌呤黄嘌呤氧化酶 (XO)抑制剂,Ki值为 0.6 nM。Febuxostat sodium 具有研究高尿酸血症和痛风的潜力。
产品描述
Febuxostat (TEI 6720) sodium is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a K i value of 0.6 nM. Febuxostat sodium has the potential for the research of hyperuricemia and gout [1] [2] [3].
体外活性
Febuxostat sodium 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].
体内活性
Febuxostat sodium (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 sodium (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 sodium (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 sodium (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 sodium (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].
Cas No.
1140907-13-6
分子式
C16H15N2NaO3S
分子量
338.36
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years