Tenatoprazole sodium
Tenatoprazole sodium (TU-199 sodium) is a proton pump inhibitor; inhibits hog gastric H+/K+-ATPase with an IC50 of 6.2 μM.
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- CAS. Nr.: 335299-59-7
- Formel: C16H17N4NaO3S
- Molecular Weight:368.39
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
IC50: 6.2 μM (H+/K+-ATPase)[1]
Tenatoprazole inhibits hog gastric H+/K+-ATPase activity with almost equal potency to that of omeprazole (IC50=6.2 and 4.2 microM, respectively)[1]. Tenatoprazole is a prodrug of the proton pump inhibitor class. Tenatoprazole is converted to the active sulfenamide or sulfenic acid by acid in the secretory canaliculus of the stimulated parietal cell of the stomach. This active species binds to luminally accessible cysteines of the gastric H+/K+-ATPase resulting in disulfide formation and acid secretion inhibition. Tenatoprazole binds at the catalytic subunit of the gastric acid pump with a stoichiometry of 2.6 nmol/mg of the enzyme[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 335299-59-7
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Molecular Weight 368.39
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Formel C16H17N4NaO3S
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SMILES
O=S(C1=NC2=CC=C(OC)N=C2[N-]1)CC3=NC=C(C)C(OC)=C3C.[Na+]
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Synonyms
TU-199 sodium
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
The enzyme suspension (20 mg/mL) is incubated at 37°C in a buffer composed of 5 mM Pipes/Tris (pH 6.95), 2 mM MgCl2, 150 mM KCl, 3 mg/mL of valinomycin, 1 mM acridine orange, in the presence of 0.1 mM glutathione, in a SPEX spectrofluorometer for 5 min. Inhibitor (20 mM), omeprazole or tenatoprazole, is added and fluorescence is measured by excitation at 490 nm and emission at 530 nm. After 60 s, ATP (2 mM) is added to initiate acridine orange uptake as a measure of intra-vesicular acidification[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats: (R,S)-Tenatoprazole free form (50 mg/kg) or (S)-tenatoprazole sodium salt hydrate (50 mg/kg) is orally administered to dogs and the plasma level of tenatoprazole is measured as a function of time course. Similarly, (S)-tenatoprazole free form (100 mg/kg) or (S)-tenatoprazole sodium salt hydrate (100 mg/kg) is orally administered to dogs and the plasma level of tenatoprazole is measured as a function of time[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)