Topiroxostat

577778-58-6

248.24

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

Metabolic Enzyme/Protease; Metabolic Enzyme/Protease

Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC₅₀ value of 5.3 nM and a K_i 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] 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]. 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_max and bioavailability of Topiroxostat (FYX-051, compound 39) are as high as 4.62 ug/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t_1/2 value of Topiroxostat is 19.7 hours^[1].