577778-58-6

• 常用中文名：托匹司他
• 常用英文名：Topiroxostat
• CAS号：577778-58-6
• 分子式：C₁₃H₈N₆
• 分子量：248.243
• 相关类别： 信号通路 代谢酶/蛋白酶 黄嘌呤氧化酶
• 发布时间：2018-03-24 08:00:00
• 更新时间：2026-07-02 08:29:29
• Topiroxostat(FYX-051)是黄嘌呤氧化还原酶（XOR）抑制剂，IC50为5.3 nM。

名称

• 中文名: 托比司他
• 英文名: 4-(5-pyridin-4-yl-1H-1,2,4-triazol-3-yl)pyridine-2-carbonitrile
• 中文别名: 4-(5-(吡啶-4-基)-1H-1,2,4-三唑-3-基)皮考啉腈; 托普司他; 托匹司他精制; 托匹司他,10 MM DMSO 溶液; 2-氰基-N' - [(吡啶-4-基)羧酰亚胺基]吡啶-4-碳酰肼; 4-(3-吡啶-4-基-1H-1,2,4-三唑-5-基)吡啶-2-腈; 托匹司特; 托洛司它; 罗恩 托比司他 R051952; 托普司他/托匹司他; 托吡司他; 4-[5-(4-吡啶基)-1H-1,2,4-三唑-3-基]吡啶-2-甲腈; 托吡司特 Topiroxostat; 托吡司特及杂质; 托匹司他/托吡司特; 4-(3-(吡啶-4-基)-1H-1,2,4-三唑-5-基)吡啶腈; 托比司他/托匹司他; TOPIROXOSTAT 托匹司他 FYX-051; 托吡司特; 托吡司特及中间体、杂质; 托比斯特; 氘4-托匹罗司; 4-(5-吡啶-4-基-1H-1,2,4-三唑-3-基)吡啶-2-甲腈; 托吡司他(托匹司他); 托匹司他577-6; 托吡酮; 抑制剂Topiroxostat
• 英文别名: 3-(3-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole; Topiroxostat,FYX-051; 5-(2-Cyano-4-pyridyl)-3-(4-pyridyl)-1,2,4-triazole; Uriadec (TN); Toby Str; [14C]-Topiroxostat; 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile; FYX-051; FYX051; FYX 051; TOPIROXOSTAT. TRADE NAMES TOPILORIC; URIADEC; 4-[5-(4-pyridinyl)-1H-1,2,4-triazol-3-yl]-2-Pyridinecarbonitrile; Topiroxostat. trade names Topiloric; 4-[5-(4-Pyridyl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile; Topiester; N-desmethyl N-Nitroso Topotecan-D3; Uriadec; 4-(5-(pyridin-4-yl)-1h-1,2,4-triazol-3-yl)picolinonitrile; Topiroxostat C13H8N6 high quality Cas number：577-6; Topiroxostat, 10 mM in DMSO; 4-[3-(4-Pyridinyl)-1H-1,2,4-triazol-5-yl]-2-pyridinecarbonitrile; FYX 051; D4-Topiroxostat; 4-(3-(Pyridin-4-yl)-1H-1,2,4-triazol-5-yl)picolinonitrile; 4-(3-(Pyridin-4-yL; 4-[5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile; Topicast impurity; Topiroxosta; Topiloric; Topiroxostat [INN]; 2-Pyridinecbonitrile, 4-[5-(4-pyridinyl)-1H-1,2,4-triazol-3-yl]; Topiroxostat impurty; Topiroxostat 5-(2-Cyano-4-pyridyl)-3-(4-pyridyl)-1,2,4-triazole; 2-Pyridinecbonitrile, 4-[3-(4-pyridinyl)-1H-1,2,4-triazol-5-yl]; Factory supply Topiroxostat Cas 577-6 with high quality and best price; inonitriL

物化性质

• 密度: 1.5±0.1 g/cm3
• 沸点: 594.7±60.0 °C at 760 mmHg
• 分子式: C₁₃H₈N₆
• 分子量: 248.243
• 闪点: 175.3±18.1 °C
• 精确质量: 248.081039
• PSA: 91.14000
• LogP: 1.35
• 蒸汽压: 0.0±1.7 mmHg at 25°C
• 折射率: 1.697
• 储存条件: 室温，干燥

生物活性

• 描述: Topiroxostat(FYX-051)是黄嘌呤氧化还原酶(XOR)抑制剂,IC50为5.3 nM。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 黄嘌呤氧化酶
  研究领域 >> 代谢疾病
• 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]. Shimo T, et al. Xanthine crystals induced by topiroxostat, a xanthine oxidoreductase inhibitor, in rats, cause transitional cell tumors. Arch Toxicol. 2014 Jan 22.

  [3]. 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.

合成路线

100-48-1 135048-32-7 ~% 577778-58-6

文献：EP1471065 A1, ; Page 8 ;

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