Tegoprazan is an orally active, highly selective gastric H+/K+-ATPase inhibitor that controls gastric acid secretion and motility, with an IC50 of 0.29-0.52 μM for porcine, canine, and human H+/K+-ATPase in vitro.

H+, K+-ATPase:0.29-0.52 μM

METHODS: BMM cells were cultured with Tegoprazan (CJ-12420) (0, 0.0005, 0.001, 0.005, 0.01, 0.05, 0.1, 0.5, 1, 10, 100 and 1000 μg/mL, 24 hours) to investigate its effects on BMM cytotoxicity and nitric oxide (NO) production.
RESULTS When the concentration of Tegoprazan was 0.5, 1, 10 and 100 μg/mL, the cell viability exceeded 80%; when the concentration was 1000 μg/mL, the cell viability was less than 80%; 100 μg/mL of Tegoprazan could significantly inhibit NO production in BMM cells. [3]

METHODS: Tegoprazan (CJ-12420) (3, 10 mg/kg, oral, 5 days) was used to treat pylorus-ligated rats, and the effects of Tegoprazan and esomeprazole on gastric acid secretion in pylorus-ligated rats were observed.
RESULTS The gastric fundus pH values ​​of 3 mg/kg Tegoprazan were 4.13 and 4.34, respectively, and the gastric fundus pH values ​​of 10 mg/kg Tegoprazan were 6.86 and 6.63, respectively. Tegoprazan can completely inhibit gastric acid secretion. [3]