Tenatoprazole 是一种口服有效的，基于咪唑吡啶的质子泵抑制剂。它抑制猪胃H+/K+-ATP 酶活性，IC50为6.2 μM。它阻断泛素与 ESCRT-1 因子 Tsg101 的相互作用，抑制几种包膜病毒的产生，包括 EBV。

Tenatoprazole, a prodrug of the proton pump inhibitor (PPI) class, can inhibit proton transport (IC50: 3.2 μM).

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]

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]

113712-98-4

C16H18N4O3S

346.41

泰妥拉唑;TU-199

DMSO:43 mg/mL (124.1 mM)
Ethanol:12 mg/mL (34.6 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years