CAS 78090-11-6|Picoprazole

Introduction:Basic information about CAS 78090-11-6|Picoprazole, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NamePicoprazole
CAS Number78090-11-6Molecular Weight343.40000
Density1.41g/cm3Boiling Point597.1ºC at 760 mmHg
Molecular FormulaC17H17N3O3SMelting Point/
MSDS/Flash Point314.9ºC

Names

Namemethyl 6-methyl-2-[(3-methylpyridin-2-yl)methylsulfinyl]-1H-benzimidazole-5-carboxylate
SynonymMore Synonyms

Picoprazole BiologicalActivity

DescriptionPicoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1±0.4 μM.
Related CatalogSignaling Pathways >>Membrane Transporter/Ion Channel >>Proton PumpResearch Areas >>Metabolic Disease
Target

IC50: 3.1±0.4 μM (H+/K+-ATPase)[1]

In VitroPicoprazole 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

Density1.41g/cm3
Boiling Point597.1ºC at 760 mmHg
Molecular FormulaC17H17N3O3S
Molecular Weight343.40000
Flash Point314.9ºC
Exact Mass343.09900
PSA104.15000
LogP3.53480
Index of Refraction1.684
InChIKeyASSMECARUIRCML-UHFFFAOYSA-N
SMILESCOC(=O)c1cc2nc(S(=O)Cc3ncccc3C)[nH]c2cc1C
Storage condition2-8℃

Synonyms

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