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

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

目錄號(hào): HY-14874 純度: 99.63%
COA 產(chǎn)品使用指南

Topiroxostat (FYX-051) 是一種有效的口服黃嘌呤氧化還原酶 (XOR) 抑制劑，IC50 值為 5.3 nM，Ki 值為 5.7 nM。Topiroxostat 還表現(xiàn)出弱的 CYP3A4 抑制活性 (18.6%)。Topiroxostat 有潛力用于高尿酸血癥的研究。

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Topiroxostat Chemical Structure

Topiroxostat Chemical Structure

CAS No. : 577778-58-6

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規(guī)格 價(jià)格 是否有貨 數(shù)量
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   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Topiroxostat:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]
體外研究
(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.
體內(nèi)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 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

托匹司他
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 23.5 mg/mL (94.67 mM; 超聲加熱助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
Topiroxostat
目錄號(hào)：
HY-14874
需求量：