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首页 / 抑制剂/激动剂 / 代谢酶 / 黄嘌呤氧化酶 / Febuxostat

非布司他 /Febuxostat {[allProObj[0].p_purity_real_show]}

货号：A274351 同义名： 非布索坦 / TEI 6720;TMX 67

Febuxostat is an inhibitor of xanthine oxidase with Ki of 0.6 nM and can affect the progression of renal disease.

Febuxostat 化学结构 CAS号：144060-53-7
Febuxostat 化学结构
CAS号：144060-53-7
Febuxostat 3D分子结构
CAS号：144060-53-7
Febuxostat 化学结构 CAS号：144060-53-7
Febuxostat 3D分子结构 CAS号：144060-53-7
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Febuxostat 纯度/质量文件 产品仅供科研

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Febuxostat 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].

Febuxostat 动物研究

Dose Rat: 1 mg/kg - 10 mg/kg[3] (p.o.) Mice: 1 mg/kg, 5 mg/kg[4] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Mice[5]
Dose 24 mg/kg
Administration p.o.
Cmax 19672.3 ng/ml (day 1)
32350.5 ng/ml (week 19)
Tmax 0.5 h (day 1)
0.5 h (week 19)
AUC0→24h 31187.6 ng·h/ml (day 1)
36519.2 ng·h/ml (week 19)

Febuxostat 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 - -

Febuxostat 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.

Febuxostat 实验方案

计算器
存储液制备 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

Febuxostat 技术信息

CAS号144060-53-7
分子式C16H16N2O3S
分子量 316.37
别名 非布索坦 ;TEI 6720;TMX 67;Adenuric;Uloric;FBX
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

Tags: Febuxostat | TEI 6720;TMX 67;Adenuric;Uloric;FBX | 非布索坦 | Xanthine Oxidase | AmBeed-信号通路专用抑制剂 | Febuxostat 纯度/质量文件 | Febuxostat 生物活性 | Febuxostat 动物研究 | Febuxostat 临床数据 | Febuxostat 参考文献 | Febuxostat 实验方案 | Febuxostat 技术信息

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