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CAS No.: 577778-58-6

Topiroxostat/托匹司他 Catalog No. CSN19437

Synonyms: FYX-051;托匹司他

Topiroxostat is an inhibitor of xanthine oxidoreductase (XOR) with IC50 of 5.3 nM.

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技术信息

生物活性

描述Xanthine oxidoreductase (XOR) belongs to the group of molybdenum-containing hydroxylases involved in the oxidative metabolism of purines. Xanthine oxidoreductase is a key enzyme in purine degradation. It catalyzes the oxidation of hypoxanthine to xanthine and the oxidation of xanthine to uric acid. Xanthine oxidoreductase contributes to the generation of reactive oxygen species. Topiroxostat, also termed FYX-051, is a XOR inhibitor with IC₅₀ value of 5.3 nM in an in vitro assay^[3]. Steady-state kinetics study showed that topiroxostat behaved as a competitive-type inhibitor with a Ki value of 5.7 × 10 nM^[4]. Oral administration of Topiroxostat at doses ranging in 0.03-1mg/kg dose-dependently decreased serum urate levels in oxonate-induced hyperuricemic rats, with ED₅₀ values of 0.15 mg/kg, 0.25 mg/kg and 0.70 mg/kg at 1h, 6h, and 12h^[4]. Oral administration of Topiroxostat at doses of 0.1, 0.3, 1 and 3 mg/kg/day for 4 weeks dose-dependently decreased the urinary albumin excretion, inhibited plasma XOR activity in diabetic mice model^[5].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02837198	Hyperuricemia	Phase 2	Completed	-	Japan ... more >> Tokyo, Japan Collapse <<
NCT02327754	Diabetic Nephropathy	Phase 2	Completed	-	Japan ... more >> Sanwa Kagaku Kenkyusho Co., Ltd. Nagoya, Aichi, Japan, 461-8631 Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0283 mL
- 20.1416 mL
- 40.2831 mL
- 5 mM
- 0.8057 mL
- 4.0283 mL
- 8.0566 mL
- 10 mM
- 0.4028 mL
- 2.0142 mL
- 4.0283 mL

技术信息

CAS号

577778-58-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H8N6

运输

蓝冰

分子量

248.24

别名

FYX-051;托匹司他

溶解度

DMSO	40.0 mg/mL (161.1 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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