881681-00-1

• 常用中文名：沃诺拉赞
• 常用英文名：Vonoprazan
• CAS号：881681-00-1
• 分子式：C₁₇H₁₆FN₃O₂S
• 分子量：345.391
• 相关类别： 原料药 消化系统用药 抗酸及胃黏膜保护药
• 发布时间：2018-02-16 08:00:00
• 更新时间：2026-07-02 20:26:41
• TAK-438 (free base)是一种新型的钾竞争性的酸阻断剂,可逆抑制H+/K+,ATPase,IC50为19 nM (pH 6.5)。

名称

• 中文名: 凡诺帕胺
• 英文名: Vonoprazan
• 中文别名: 沃诺拉赞间氟异构体; 沃诺拉赞/伏诺拉生; 沃诺拉赞标准品025; 文诺普兰标准品025; 沃诺拉赞杂质; 伏诺拉赞; 沃诺拉赞游离碱; 沃诺拉赞相关杂质29; (2-氟苯基)-N-甲基-1-(3-吡啶基磺酰基)-1H-吡咯-3-甲胺; 沃诺拉赞杂质二聚体; 富马酸沃诺他赞; 文诺普兰,沃诺拉赞; TAK438杂质39; 富马酸沃诺拉赞中间体3; 1-[5-(2-氟苯基)-1-(吡啶-3-磺酰基)-1H-吡咯-3-基]-N-甲基甲胺(沃诺拉赞杂质); 沃诺拉赞,10 MM DMSO 溶液; TAK438中间体 6; 1-(5-(2-氟苯基)-1-(吡啶-3-基磺酰基)-1H-吡咯-3-基)-N-甲基甲胺; 沃诺拉赞标准品; 伏诺拉生BASE; 5-(2-氟苯基)-N-甲基-1-(3-吡啶基磺酰基)-1H-吡咯-3-甲胺; 伏诺拉生标准品025; 伏诺拉生/沃诺拉赞
• 英文别名: Vonoprazan free base; 1- [5- (2-Fluorophenyl)-1- (pyridine-3-sulfonyl)-1H-pyrrol-3-yl] N-methylmethanamine; TAK-438; TAK-438 free base (Vonoprazan; 1H-Pyrrole-3-methanamine,5-(2-fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl); TAK438 Intermediate 6; 1-[5-(2-Fluorophenyl)-1-[(pyridin-3-yl)sulfonyl]-1H-pyrrol-3-yl]-N-methylmethanamine; Vonoprazan (Vonoprazan Impurity); 5-(2-Fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-1H-pyrrole-3-methanamine; Vonoprazan Impurity; Vonoprazan //BP; 1-[5-(2-Fluorophenyl)-1-(3-pyridinylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine; Voronazan interfluoroisomer; Vonoprazan, 10 mM in DMSO; Vonoprazan-025; Vonoprazan m-Fluoro Isomer; Vonoprazan related Impuirty 29; Vonopraza/Vonoprazan fumate; TAK438 Impurity; TAK-438 (free base)

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 530.3±60.0 °C at 760 mmHg
• 分子式: C₁₇H₁₆FN₃O₂S
• 分子量: 345.391
• 闪点: 274.5±32.9 °C
• 精确质量: 345.094727
• LogP: 2.74
• 蒸汽压: 0.0±1.4 mmHg at 25°C
• 折射率: 1.622

生物活性

• 描述: TAK-438 (free base)是一种新型的钾竞争性的酸阻断剂,可逆抑制H+/K+,ATPase,IC50为19 nM (pH 6.5)。
• 相关类别:
  信号通路 >> 跨膜转运 >> 质子泵
  研究领域 >> 内分泌
• 参考文献:

  [1]. Arikawa Y, et al. Discovery of a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB). J Med Chem, 2012, 55(9), 4446-4456.

  [2]. Hori Y, et al. 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438), a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases. J Pharmacol Exp Ther, 2010, 335(1), 231-238.

  [3]. Hori Y, et al. A study comparing the antisecretory effect of TAK-438, a novel potassium-competitive acid blocker, with lansoprazole in animals. J Pharmacol Exp Ther, 2011, 337(3), 797-804.