TY-11345

TY-11345 is an orally active gastric mucosal H⁺/K⁺-ATPase inhibitor, with IC₅₀ values of 5.8 μM (Reference 1) and 3.3 μM (Reference 2) at pH 6.0, respectively. TY-11345 inhibits basal gastric acid secretion stimulated by Tetragastrin (HY-125556) and Pentagastrin (HY-A0261), and prevents gastric and duodenal injuries in rats. TY-11345 can be used in the research of peptic ulcer disease and acid-related gastrointestinal diseases^[1][2]. In Vitro:TY-11345 potently inhibits ^H+/K⁺-ATPase activity in purified rabbit gastric mucosal microsomes, with an IC₅₀ of 5.8 μM at pH 6.0 and 9.9 μM at pH 7.4; furthermore, it achieves near-maximal inhibitory effect within 10 min of pre-incubation at pH 6.0^[1].
TY-11345 potently inhibits H⁺/K⁺-ATPase isolated from rabbit gastric mucosa, with an IC₅₀ value of 3.3 μM at pH 6.0 and 9.7 μM at pH 7.4^[2]. In Vivo:TY-11345 (0.3-1.0 mg/kg; intravenous injection; single dose) potently inhibits tetragastrin-stimulated gastric acid secretion in rats, with an ED₅₀ of 0.22 mg/kg during the 150 to 180-minute period^[1].
TY-11345 (0.1-100 mg/kg; intravenous, intradermal, oral administration; single dose) potently inhibits basal gastric acid secretion in pylorus-ligated rats via multiple routes, with an ED₅₀ of 1.2 mg/kg following duodenal administration^[1].
TY-11345 (0.3-3.0 mg/kg; p.o.; single administration) potently prevents water immersion stress-induced gastric injury in rats, with an ED₅₀ of 0.92 mg/kg^[1].
TY-11345 (0.3-3.0 mg/kg; p.o.; single administration) potently prevents Indomethacin (HY-14397)-induced gastric injury in rats, with an ED₅₀ of 0.64 mg/kg^[1].
TY-11345 (3-30 mg/kg; p.o.; single administration) potently prevents Ethanol-induced gastric injury in rats, with an ED₅₀ of 10.5 mg/kg^[1].
TY-11345 (0.3-3.0 mg/kg; p.o.; twice-daily dosing) potently prevents mepirizole (HY-103595)-induced duodenal ulcers in rats, with an ED₅₀ of 0.90 mg/kg^[1].
TY-11345 (3-30 mg/kg; p.o.; once daily; 14 days) potently promotes the healing of chronic gastric ulcers induced by Acetic acid (HY-Y0319) in rats, with an ED₅₀ of 16.5 mg/kg/day^[1].
TY-11345 (1 mg/kg; intravenous injection; single administration) achieves a maximum inhibition rate of 67.1% against pentagastrin-stimulated gastric acid secretion in rats, and maintains an inhibitory effect of 54.9% at 3 h post-administration^[2].