Description
Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1±0.4 μM.
Product information
CAS Number: 78090-11-6
Molecular Weight: 343.40
Formula: C17H17N3O3S
Chemical Name: methyl 5-methyl-2-[(3-methylpyridin-2-yl)methanesulfinyl]-1H-1,3-benzodiazole-6-carboxylate
Smiles: CC1C=C2N=C(NC2=CC=1C(=O)OC)S(=O)CC1=NC=CC=C1C
InChiKey: ASSMECARUIRCML-UHFFFAOYSA-N
InChi: InChI=1S/C17H17N3O3S/c1-10-5-4-6-18-15(10)9-24(22)17-19-13-7-11(2)12(16(21)23-3)8-14(13)20-17/h4-8H,9H2,1-3H3,(H,19,20)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Picoprazole inhibits the H+/K+-ATPase activity in a concentration-dependent manner. The IC50 value is 3.1±0.4 μM. 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. 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.
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