Tenatoprazole

Catalog No.S4212 Synonyms: TU-199

For research use only.

Tenatoprazole (TU-199) is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 μM. Tenatoprazole labels only the gastric H(+),K(+)-ATPase alpha-subunit, approximately 2.6 nM/mg of tenatoprazole is bound to the H(+),K(+)-ATPase.

Tenatoprazole Chemical Structure

CAS No. 113712-98-4

Selleck's Tenatoprazole has been cited by 1 Publication

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Biological Activity

Description Tenatoprazole (TU-199) is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 μM. Tenatoprazole labels only the gastric H(+),K(+)-ATPase alpha-subunit, approximately 2.6 nM/mg of tenatoprazole is bound to the H(+),K(+)-ATPase.
Targets
Proton pump [1]
()
H(+),K(+)-ATPase [1]
(Cell-free assay)
3.2 μM
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 (from reference)

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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CN=C(C(=C1OC)C)CS(=O)C2=NC3=C(N2)C=CC(=N3)OC

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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.

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