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S85842

Topiroxostat

源叶(MedMol) 98%
  • 英文名:
  • Topiroxostat
  • 别名:
  • CAS号:
  • 577778-58-6
  • 分子式:
  • C13H8N6
  • 分子量:
  • 248.2428
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S85842-5mg 98% ¥280.00元 >10 - - - EA 加入购物车
源叶(MedMol) S85842-10mg 98% ¥400.00元 >10 2 - - EA 加入购物车
源叶(MedMol) S85842-50mg 98% ¥1200.00元 >10 - - - EA 加入购物车
源叶(MedMol) S85842-100mg 98% ¥1520.00元 >10 - - - EA 加入购物车
源叶(MedMol) S85842-250mg 98% ¥2800.00元 >10 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: 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
  • 靶点: IC50: 5.3 nM (XOR) Ki: 5.7 nM (XOR);P450;ROS;XanthineOxidase
  • 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
  • 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.
  • 参考文献:
    1. Sato T, et al. Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia [corrected]. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6225-9. 2. Matsumoto K, et al. FYX-051: a novel and potent hybrid-type inhibitor of xanthine oxidoreductase. J Pharmacol Exp Ther. 2011 Jan;336(1):95-103.
  • 溶解性: soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 4.028 ml 20.142 ml 40.283 ml
    5 mM 0.806 ml 4.028 ml 8.057 ml
    10 mM 0.403 ml 2.014 ml 4.028 ml
    50 mM 0.081 ml 0.403 ml 0.806 ml
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