Picoprazole
Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1±0.4 μM.
For research use only. We do not sell to patients.
- CAS No.: 78090-11-6
- Formula: C17H17N3O3S
- Molecular Weight:343.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 78090-11-6
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Molecular Weight 343.40
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Formula C17H17N3O3S
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SMILES
O=C(C1=C(C)C=C2N=C(S(CC3=NC=CC=C3C)=O)NC2=C1)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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. [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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)