product name Tenatoprazole
Description: Tenatoprazole, also known as TU-199, is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 μM. Tenatoprazole, is a drug candidate that was undergoing clinical testing as a potential treatment for reflux oesophagitis and peptic ulcer. Tenatoprazole has an imidazopyridine ring in place of the benzimidazole moiety found in other proton pump inhibitors, and has a half-life about seven times longer than other PPIs.
References: Biochem Pharmacol. 2006 Mar 14;71(6):837-49.
346.4
Formula
C16H18N4O3S
CAS No.
113712-98-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 46 mg/mL (132.8 mM)
Water: <1 mg/mL
Ethanol: 14 mg/mL (40.4 mM)
Solubility (In vivo)
Synonyms
TU-199
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Biochem Pharmacol. 2006 Mar 14;71(6):837-49. |
