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Febuxostat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Febuxostat图片
CAS NO:144060-53-7

非布司他
TEI 6720
TMX 67
Febuxostat (TEI 6720) 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 具有研究高尿酸血症和痛风的潜力。
生物活性

Febuxostat (TEI 6720) is a potent, selective and non-purinexanthine oxidase(XO)inhibitor with aKivalue of 0.6 nM. Febuxostat has the potential for the research of hyperuricemia and gout[1][2][3].

IC50& Target

Ki: 0.6 nM (Xanthine oxidase)[1]

体外研究
(In Vitro)

Febuxostat displays potent mixed-type inhibition of the activity of purified bovine milk xanthine oxidase, with Kiand Ki' values of 0.6 nM and 3.1 nM respectively, indicating inhibition of both the oxidized and reduced forms of xanthine oxidase[1].

体内研究
(In Vivo)

Febuxostat (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 (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 (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 (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 (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].

Clinical Trial
分子量

316.37

性状

Solid

Formula

C16H16N2O3S

CAS 号

144060-53-7

中文名称

非布司他

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL(158.04 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.1609 mL15.8043 mL31.6086 mL
5 mM0.6322 mL3.1609 mL6.3217 mL
10 mM0.3161 mL1.5804 mL3.1609 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.90 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。
 
 
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