2. Metabolic Enzyme/Protease
  3. Xanthine Oxidase Cytochrome P450
  4. Topiroxostat

Topiroxostat  (Synonyms: 托匹司他; FYX-051)

目录号: HY-14874 纯度: 99.63%
COA 产品使用指南

摩尔计算器

Topiroxostat (FYX-051) 是一种有效的口服黄嘌呤氧化还原酶 (XOR) 抑制剂，IC50 值为 5.3 nM，Ki 值为 5.7 nM。Topiroxostat 还表现出弱的 CYP3A4 抑制活性 (18.6%)。Topiroxostat 有潜力用于高尿酸血症的研究。

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Topiroxostat Chemical Structure

Topiroxostat Chemical Structure

CAS No. : 577778-58-6

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥330
In-stock
5 mg ￥300
In-stock
10 mg ￥480
In-stock
25 mg ￥864
In-stock
50 mg ￥1296
In-stock
100 mg ￥1944
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Topiroxostat:

Topiroxostat 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment[1][2].

IC50 & Target

IC50: 5.3 nM (XOR)[1]
Ki: 5.7 nM (XOR)[2]
体外研究
(In Vitro)

These potent and more sustained effects of Topiroxostat (FYX-051, compound 39) have been confirmed by a crystallographic analysis of XOR-Topiroxostat complex. The cyano group of Topiroxostat has been reported to play an important role in the binding activity between Topiroxostat and XOR. This is attributable to the formation of a hydrogen bond between Asn 768 of XOR and the cyano group of Topiroxostat[1].

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

Topiroxostat 相关抗体:
体内研究
(In Vivo)

Topiroxostat (FYX-051; 0.03-10 mg/kg; oral administration; for 1 hour; male Wistar/ST strain rats) treatment shows a potent and long-lasting hypouricemic effect in a rat model of potassium oxonate-induced hyperuricemia[2] .
The Cmax and bioavailability of Topiroxostat (FYX-051, compound 39) are as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t1/2 value of Topiroxostat is 19.7 hours[1].

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

Animal Model: Male Wistar/ST strain rats (7 weeks old) injected with potassium oxonate[2]
Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: Oral administration; for 1 hour
Result: Caused a dose-dependent decrease in serum urate levels with an extremely low ED50 of 0.15 mg/kg, evaluated at 1 h after oral administration.
Clinical Trial
分子量

248.24

Formula

C13H8N6
CAS 号
性状

固体

颜色

White to off-white

中文名称

托匹司他
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 23.5 mg/mL (94.67 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.0284 mL 20.1418 mL 40.2836 mL
5 mM 0.8057 mL 4.0284 mL 8.0567 mL
查看完整储备液配制表

* 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°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Topiroxostat 相关分类

完整储备液配制表

* 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°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.0284 mL 20.1418 mL 40.2836 mL 100.7090 mL
5 mM 0.8057 mL 4.0284 mL 8.0567 mL 20.1418 mL
10 mM 0.4028 mL 2.0142 mL 4.0284 mL 10.0709 mL
15 mM 0.2686 mL 1.3428 mL 2.6856 mL 6.7139 mL
20 mM 0.2014 mL 1.0071 mL 2.0142 mL 5.0354 mL
25 mM 0.1611 mL 0.8057 mL 1.6113 mL 4.0284 mL
30 mM 0.1343 mL 0.6714 mL 1.3428 mL 3.3570 mL
40 mM 0.1007 mL 0.5035 mL 1.0071 mL 2.5177 mL
50 mM 0.0806 mL 0.4028 mL 0.8057 mL 2.0142 mL
60 mM 0.0671 mL 0.3357 mL 0.6714 mL 1.6785 mL
80 mM 0.0504 mL 0.2518 mL 0.5035 mL 1.2589 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Topiroxostat577778-58-6FYX-051托匹司他FYX051FYX 051Xanthine OxidaseCytochrome P450XOCYPsXORAsn 768uricacidhyperuricemiaCYP3A4pharmacokineticInhibitorinhibitorinhibit

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