吡考拉唑
- CAS号:78090-11-6
- 英文名:Picoprazole
- 中文名:吡考拉唑
- CBNumber:CB81179493
- 分子式:C17H17N3O3S
- 分子量:343.4
- MOL File:78090-11-6.mol
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
吡考拉唑性质、用途与生产工艺
- 生物活性 Picoprazole 是一种特异性的 H+/K+-ATPase 抑制剂,IC50 为 3.1±0.4 μM。
-
靶点
IC50: 3.1±0.4 μM (H + /K + -ATPase)
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体外研究
Picoprazole inhibits the H + /K + -ATPase activity in a concentration-dependent manner. The IC 50 value is 3.1±0.4 μM. Picoprazole is a specific inhibitor of H + /K + -ATPase and binds to 100-kDa polypeptides of the enzyme, dose dependently inhibited opening of the Cl - conductance by Cu 2+ -o-phenanthroline, indicating that the Cl - conductance is part of the function of the H + /K + -ATPase. The inhibitory effect of the three benzimidazole derivatives Timoprazole, Picoprazole, and Omeprazole on histamine and dbcAMP stimulated 14 C-aminopyrine accumulation (H + secretion) has been studied in isolated and enriched guinea-pig parietal cells. All compounds tested inhibit H + secretion in a concentration dependent manner with IC 50 values of 8.5±1.9 μM for Timoprazole, 3.9±0.7 μM for Picoprazole, and 0.13±0.03 μM for Omeprazole.
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