产品
编 号：F395399
分子式：C13H8N6
分子量：248.24
分子式：C13H8N6
分子量：248.24
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
240
In-stock
10mg
384
In-stock
25mg
692
In-stock
50mg
1037
In-stock
100mg
1556
In-stock
结构图
CAS No: 577778-58-6
产品详情
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.
体内研究：
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 .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.Animal Model:Male Wistar/ST strain rats (7 weeks old) injected with potassium oxonate
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.
体外研究：
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.
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.
体内研究：
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 .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.Animal Model:Male Wistar/ST strain rats (7 weeks old) injected with potassium oxonate
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.
体外研究：
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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备