Picoprazole  (Synonyms: 吡考拉唑)

Picoprazole is a specific inhibitor of H⁺/K⁺-ATPase with IC₅₀ of 3.1±0.4 μM.

IC50: 3.1±0.4 μM (H⁺/K⁺-ATPase)^[1]

Picoprazole inhibits the H⁺/K⁺-ATPase activity in a concentration-dependent manner. The IC₅₀ value is 3.1±0.4 μM^[1]. 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 Cu²⁺-o-phenanthroline, indicating that the Cl^- conductance is part of the function of the H⁺/K⁺-ATPase^[2]. The inhibitory effect of the three benzimidazole derivatives Timoprazole, Picoprazole, and Omeprazole on histamine and dbcAMP stimulated ¹⁴C-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 IC₅₀ values of 8.5±1.9 μM for Timoprazole, 3.9±0.7 μM for Picoprazole, and 0.13±0.03 μM for Omeprazole^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

343.40

C₁₇H₁₇N₃O₃S

78090-11-6

吡考拉唑

Room temperature in continental US; may vary elsewhere.

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

• [1]. Beil W, et al. Inhibition of partially purified H⁺/K⁺-ATPase from guinea-pig isolated and enriched parietal cells by substituted benzimidazoles. Br J Pharmacol. 1984 Jul;82(3):651-7.  [Content Brief]

  [2]. Takeguchi N, et al. Disulfide cross-linking of H,K-ATPase opens Cl- conductance, triggering proton uptake in gastric vesicles. Studies with specific inhibitors. J Biol Chem. 1986 Feb 25;261(6):2560-6.  [Content Brief]

  [3]. Sewing KF, et al. Effect of substituted benzimidazoles on acid secretion in isolated and enriched guinea pig parietal cells. Gut. 1983 Jun;24(6):557-60.  [Content Brief]