Topiroxostat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Topiroxostat(FYX-051) 是一种新型、有效的黄嘌呤氧化还原酶 (XOR) 抑制剂，IC50 值为 5.3 nM。

Topiroxostat(FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.(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.(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 .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.

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; 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.

FYX-051

Immunology/Inflammation

ROS

XO

Metabolic Disease

——

577778-58-6

248.24

C13H8N6

>98% (HPLC)

DMSO: 10 mM

N#CC1=NC=CC(C2=NNC(C3=CC=NC=C3)=N2)=C1

4-(5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl)picolinonitrile

(-20℃)

With Ice Pack

≥ 2 years