Picoprazole

Modify Date: 2024-01-11 19:02:14

Picoprazole Structure
Picoprazole structure
Common Name Picoprazole
CAS Number 78090-11-6 Molecular Weight 343.40000
Density 1.41g/cm3 Boiling Point 597.1ºC at 760 mmHg
Molecular Formula C17H17N3O3S Melting Point N/A
MSDS N/A Flash Point 314.9ºC

 Use of Picoprazole


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

 Names

Name methyl 6-methyl-2-[(3-methylpyridin-2-yl)methylsulfinyl]-1H-benzimidazole-5-carboxylate
Synonym More Synonyms

 Picoprazole Biological Activity

Description Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1±0.4 μM.
Related Catalog
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].
References

[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.

[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.

[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.

 Chemical & Physical Properties

Density 1.41g/cm3
Boiling Point 597.1ºC at 760 mmHg
Molecular Formula C17H17N3O3S
Molecular Weight 343.40000
Flash Point 314.9ºC
Exact Mass 343.09900
PSA 104.15000
LogP 3.53480
Index of Refraction 1.684
Storage condition 2-8℃

 Synonyms

Picoprazolum
methyl 6-methyl-2-[[(3-methyl-2-pyridyl)methyl]sulfinyl]-5-benzimidazolecarboxylate
Picoprazol
Picoprazole
Picoprazole (INN)