Home Transmembrane Transporters Proton Pump inhibitor - ATPase inhibitor Tenatoprazole

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Tenatoprazole Proton Pump inhibitor

Cat.No.S4212

Tenatoprazole (TU-199,STU-Na) is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 μM. This compound labels only the gastric H(+),K(+)-ATPase alpha-subunit, approximately 2.6 nM/mg of this chemical is bound to the H(+),K(+)-ATPase.
Tenatoprazole Proton Pump inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 346.4

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Chemical Information, Storage & Stability

Molecular Weight 346.4 Formula

C16H18N4O3S

 Storage (From the date of receipt)
CAS No. 113712-98-4 Download SDF Storage of Stock Solutions

Synonyms TU-199,STU-Na Smiles CC1=CN=C(C(=C1OC)C)CS(=O)C2=NC3=C(N2)C=CC(=N3)OC

Solubility

In vitro
Batch:

DMSO : 69 mg/mL ( (199.19 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 11 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
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 this compound is bound to the H+,K+-ATPase. The two enantiomers (R)- or (S)-tenatoprazole give the same stoichiometry of binding with 88% inhibition. This compound 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. This compound inhibits about 20–30% of enzyme activity even though acid secretion in fasting rats. This chemical provides a higher Cmax of 183 ng/mL, Tmax of 1.3 hours and AUC of 822 ng*h/mL in dog. [1]
References

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