1. Membrane Transporter/Ion Channel
  2. Na+/K+ ATPase
  3. AU-461

AU-461 是一种口服有效的、可逆的胃 H⁺/K⁺ ATP 酶 (H⁺/K⁺ ATPase) 抑制剂,其对兔源酶和猪源酶的 IC₅₀ 分别为 12.15 和 4.20 μM。AU-461 与激活的阳离子 K⁺ 竞争 (Kᵢ = 1.64 μM)。AU-461 既减少了组胺刺激的胃酸分泌,也减少了大鼠的基础胃酸分泌。AU-461 抑制乙醇或者氢氧化钠所导致的溃疡形成,且使血浆胃泌素水平恢复正常水平。AU-461 可用于研究消化性溃疡。

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AU-461

AU-461 Chemical Structure

CAS No. : 220854-06-8

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  • 生物活性

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生物活性

AU-461 is an orally active and reversible inhibitor of the gastric H⁺/K⁺ ATPase with IC₅₀ values for rabbit-derived and pig-derived enzymes are 12.15 μM and 4.20 μM respectively. AU-461 competes with activated cationic K⁺ (Kᵢ = 1.64 μM). AU-461 reduces both histamine-stimulated gastric acid secretion and basal gastric acid secretion in rats. AU-461 inhibits ulcer formation caused by ethanol or sodium hydroxide, and restores the plasma gastrin level to normal. AU-461 can be used for the study of peptic ulcers[1].

分子量

447.45

Formula

C23H24F3N3O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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产品名称:
AU-461
目录号:
HY-165498
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