Topiroxostat

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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。

CAS NO:

577778-58-6

托匹司他
FYX-051

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，K_i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 aK_ivalue 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 C_maxand bioavailability of Topiroxostat (FYX-051, compound 39) are as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t_1/2value 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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 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
10 mM	0.4028 mL	2.0142 mL	4.0284 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。