Febuxostat.|144060-53-7|(非布司他; TEI 6720; TMX 67)-陌孚医药/Medlife

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Febuxostat. (Synonyms: 非布司他; TEI 6720; TMX 67)

目录号: PC14819 纯度: ≥98%

CAS No. :144060-53-7

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PC14819-25mg	25mg	¥1009.40	请登录
PC14819-100mg	100mg	¥1960.00	请登录
PC14819-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥597.80	请登录

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中文名称

Febuxostat.

中文别名

非布索坦;2-[3-氰基-4-异丁氧基苯基]-4-甲基噻唑-5-甲酸;非布司他;非布索坦 GMP;(2R,4R)- (+)-2-(二苯基膦基甲基)-4- (二环己基膦基)-N-（叔丁氧基羰基）吡咯烷;Febuxostat 抑制剂;N-甲基-4-氨基哌啶二氢溴酸盐;非布司他杂质;非布索坦（解热镇痛）药;非布索坦标准品;非布索坦合成技术转让;非布索坦原药;非布索坦杂质;非布索坦杂质（非布司他）;高哌嗪;2-(3-氰基-4-异丁氧基苯基)-4-甲基噻唑-5-羧酸;非布索坦-A晶型;非布索坦[A晶型];2-(3-氰基-4-异丁氧基苯基)-4-甲基噻唑-5-甲酸;非布索坦 2-[3-氰基-4-异丁氧基苯基]-4-甲基噻唑-5-甲酸

英文名称

Febuxostat

英文别名

Febuxostat;Tei-6720;2-[3-Cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid;2-[3-Cyano-4-isobutoxyphenyl]-4-methylthiazole-5-carboxylic acid;2-(3-Cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic Acid;2-[3-Cyano-4-(2-methylpropoxy)phenyl]-4-methyl-5-thiazolecarboxylic Acid;TMX 67;Febuxostat impurity;2-(3-Cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylic Acid,This product is unavailable;Adenuric;Febuxostat (This product is unavailable in the U.S.);Febuxostat,This product is unavailable;TEI 6720;Uloric;UNII-101V0R1N2E;2-(3-Cyano-4-isobutoxyphenyl)-4-methyl-1,3-thiazole-5-carboxylic acid;Atenuri;2-(3-Cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylic Acid;Febuxostat 2-[3-Cyano-4-isobutoxyphenyl]-4-methylthiazole-5-carboxylic acid; 2-[3-Cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carb;Feburic;Febuxostat (Uloric);2-(3-Cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid;2-(3-CYANO-4-ISOBUTOXY-PHENYL)-4-METHYL-5-THIAZOLE-CARBOXYLIC ACID;C16H16N2O3S;101V0R1N2E;5-Thiazolecarboxylic acid, 2-(3-cyano-4-(2-methylpropoxy)

Cas No.

144060-53-7

分子式

C₁₆H₁₆N₂O₃S

分子量

316.37

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Febuxostat (TEI 6720) is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a K_i value of 0.6 nM. Febuxostat has the potential for the research of hyperuricemia and gout.

性状

Solid

IC50 & Target[1][2]

Ki: 0.6 nM (Xanthine oxidase)

体外研究(In Vitro)

Febuxostat 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.
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.
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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Takano Y, et al. Selectivity of febuxostat, a novel non-purine inhibitor of xanthine oxidase/xanthine dehydrogenase. Life Sci, 2005, 76(16), 1835-1847. [Information]

[2]. Sanchez-Lozada LG, et al. Effects of febuxostat on metabolic and renal alterations in rats with fructose-induced metabolic syndrome. Am J Physiol Renal Physiol, 2008, 294(4), F710-F718. [Information]

[3]. Sanchez-Lozada LG, 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-p78. [Information]

[4]. Nomura J, et al. Xanthine oxidase inhibition by febuxostat attenuates experimental atherosclerosis in mice. Sci Rep. 2014 Apr 1;4:4554. [Information]

[5]. Karve AV, et al. Evaluation of effect of allopurinol and febuxostat in behavioral model of depression in mice. Indian J Pharmacol. 2013 May-Jun;45(3):244-7. [Information]

[6]. Khames A, et al. Ameliorative effects of sildenafil and/or febuxostat on doxorubicin-induced nephrotoxicity in rats. Eur J Pharmacol. 2017 Jun 15;805:118-124. [Information]

溶解度数据

体外研究:

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

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1609 mL	15.8043 mL	31.6086 mL
5 mM	0.6322 mL	3.1609 mL	6.3217 mL
10 mM	0.3161 mL	1.5804 mL	3.1609 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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