产品说明书

Febuxostat

Print
Chemical Structure| 144060-53-7 同义名 : 非布索坦 ;TEI 6720;TMX 67;Adenuric;Uloric;FBX
CAS号 : 144060-53-7
货号 : A274351
分子式 : C16H16N2O3S
纯度 : 98%
分子量 : 316.37
MDL号 : MFCD00871598
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(158.04 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Xanthine oxidase (XO) is catalyzes the two terminal reactions in uric acid synthesis. The inhibitors of this enzyme have been used in the treatment of hyperuricemia and gout. Febuxostat is a non-purine inhibitor of XO that shows potent inhibition of purified bovine milk XO with Ki and Ki’ values of 0.6 and 3.1nM, respectively, indicating that febuxostat was able to inhibit both oxidized and reduced forms of XO[6]. In Sprague–Dawley rats with renal ischemia–reperfusion (I/R) injury, pretreatment of febuxostat (10 mg/kg) significantly decreased UA levels (0.3mg/dL) compared with vehicle-treated group (1.4mg/dL) 4h after the injury. Also, the concentration of a nitro-oxidative stress marker, nitrotyrosine, in febuxostat-treated I/R-injured kidneys was lower (11.9pmol/g tissue) than that from control kidney (30.7pmol/g tissue) 4h post disease induction. Febuxostat also significantly reduced TBARS concentration (28.5nmol/g tissue) compared with vehicle-treated animals (37.6nmol/g tissue). In addition, febuxostat ameliorated the induced serum UN and creatinine levels, which was seen in the control group. After the injury, the number of ED-1 positive macrophages was significantly increased in interstitial area of kidneys at 24h and 72h, while febuxostat prevented the infiltration of ED-1-positive macrophages[7].
作用机制 Febuxostat exerts potent mixed-type inhibition of XO by the high-affinity binding to the enzyme in a molecular channel leading to the molybdenum-pterin active site[8].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03691688 - Recruiting March 1, 2022 China, Shanghai ... 展开 >> Shanghai Zhongshan Hospital Recruiting Shanghai, Shanghai, China, 200032 Contact: Shalaimaiti Shali, MD    86+13761553110    shali@zs-hospital.sh.cn    Contact: Yuxiang Dai, MD,PhD    +86-13818988550    dai.yuxiang@zs-hospital.sh.cn    Principal Investigator: Junbo Ge, Professor 收起 <<
NCT01361646 Hyperuricemia ... 展开 >> Gout 收起 << Phase 1 Completed - Korea, Republic of ... 展开 >> Seoul National University Hospital Seoul, Korea, Republic of, 110-744 收起 <<
NCT01508702 Gout Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.16mL

0.63mL

0.32mL

15.80mL

3.16mL

1.58mL

31.61mL

6.32mL

3.16mL
参考文献

[1]Sanchez-Lozada LG, Tapia E, et al. Effect of febuxostat on the progression of renal disease in 5/6 nephrectomy rats with and without hyperuricemia. Nephron Physiol. 2008;108(4):p69-78.

[2]Takano Y, Hase-Aoki K, et al. Selectivity of febuxostat, a novel non-purine inhibitor of xanthine oxidase/xanthine dehydrogenase. Life Sci. 2005 Mar 4;76(16):1835-47.

[3]Shirakura T, Nomura J, et al. Febuxostat, a novel xanthine oxidoreductase inhibitor, improves hypertension and endothelial dysfunction in spontaneously hypertensive rats. Naunyn Schmiedebergs Arch Pharmacol. 2016 Aug;389(8):831-8.

[4]Yisireyili M, Hayashi M, et al. Xanthine oxidase inhibition by febuxostat attenuates stress-induced hyperuricemia, glucose dysmetabolism, and prothrombotic state in mice. Sci Rep. 2017 Apr 28;7(1):1266.

[5]TEI 6720

[6]Takano Y, Hase-Aoki K, Horiuchi H, Zhao L, Kasahara Y, Kondo S, Becker MA. Selectivity of febuxostat, a novel non-purine inhibitor of xanthine oxidase/xanthine dehydrogenase. Life Sci. 2005 Mar 4;76(16):1835-47.

[7]Tsuda H, Kawada N, Kaimori JY, Kitamura H, Moriyama T, Rakugi H, Takahara S, Isaka Y. Febuxostat suppressed renal ischemia-reperfusion injury via reduced oxidative stress. Biochem Biophys Res Commun. 2012 Oct 19;427(2):266-72.

[8]Takano Y, Hase-Aoki K, Horiuchi H, Zhao L, Kasahara Y, Kondo S, Becker MA. Selectivity of febuxostat, a novel non-purine inhibitor of xanthine oxidase/xanthine dehydrogenase. Life Sci. 2005 Mar 4;76(16):1835-47.