Picoprazole

Picoprazole is a specific inhibitor of H⁺/K⁺-ATPase with IC₅₀ of 3.1±0.4 μM. IC50 & Target: IC50: 3.1±0.4 μM (H⁺/K⁺-ATPase)^[1] In Vitro: 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].