Tenatoprazole

Catalog No.S4212 Synonyms: TU-199

Tenatoprazole Chemical Structure

Molecular Weight(MW): 346.4

Tenatoprazole is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 μM.

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Biological Activity

Description Tenatoprazole is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 μM.
Targets
Proton pump [1]
In vitro

Tenatoprazole labeled only the gastric H+,K+-ATPase alpha-subunit as has been found for other PPIs, approximately 2.6 nmol/mg of tenatoprazole is bound to the H+,K+-ATPase. The two enantiomers (R)- or (S)-tenatoprazole give the same stoichiometry of binding with 88% inhibition. Tenatoprazole labels only the peptide containing fifth and sixth transmembrane segments, these contain two cysteines, cysteine 813 in the luminal vestibule and cysteine 822 in the sixth transmembrane domain. [1]

In vivo Tenatoprazole provides slow activation in vivo, which is predicted by its chemical activation rate in fasting rats. Tenatoprazole inhibits about 20–30% of enzyme activity even though acid secretion in fasting rats. (S)-tenatoprazole sodium salt hydrate provides a higher Cmax of 183 ng/mL, Tmax of 1.3 hours and AUC of 822 ng*h/mL in dog. [1]

Protocol

Solubility (25°C)

In vitro DMSO 46 mg/mL (132.79 mM)
Ethanol 14 mg/mL warmed (40.41 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 346.4
Formula

C16H18N4O3S

CAS No. 113712-98-4
Storage powder
Synonyms TU-199

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00284908 Completed Esophagitis|Gastroesophageal Reflux|Stomach Ulcer|Duodenal Ulcer STEBA France|STEBA LABORATORIES LTD. September 2006 Phase 1
NCT00282555 Suspended Esophagitis, Reflux STEBA France February 2006 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Proton Pump Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID