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Topiroxostat
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。
Topiroxostat图片
CAS NO:577778-58-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
托匹司他
FYX-051
产品介绍
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。
生物活性

Topiroxostat (FYX-051) is a potent and orally activexanthine oxidoreductase (XOR)inhibitor with anIC50value of 5.3 nM and aKivalue of 5.7 nM. Topiroxostat exhibits weakCYP3A4-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].

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 Cmaxand bioavailability of Topiroxostat (FYX-051, compound 39) are as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t1/2value of Topiroxostat is 19.7 hours[1].

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 ED50of 0.15 mg/kg, evaluated at 1 h after oral administration.
Clinical Trial
分子量

248.24

性状

Solid

Formula

C13H8N6

CAS 号

577778-58-6

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

DMSO : 23.5 mg/mL(94.67 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.0284 mL20.1418 mL40.2836 mL
5 mM0.8057 mL4.0284 mL8.0567 mL
10 mM0.4028 mL2.0142 mL4.0284 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。