Tegoprazan

Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a reversible, orally active and highly selective inhibitor of gastric H⁺/K⁺-ATPase. Tegoprazan inhibits gastric acid secretion and motility against porcine, canine and human H⁺/K⁺-ATPase with IC₅₀ values ranging from 0.29-0.52 μM in vitro. Tegoprazan significantly improves colitis and enhances the intestinal epithelial barrier function in mice. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases^[1][2][3].
IC50 & Target:IC50: 0.29-0.52 μM (H⁺/K⁺-ATPase)^[1]. In Vitro: Tegoprazan (1.0 mM and 3.0 mM, 4 h) reduces dextran sulphate sodium (DSS)-induced colitis by maintaining high junction integrity of the epithelial mucosa in Caco-2 cells. Additionally, Tegoprazan protects the intestinal epithelial tight junction barrier and inhibits the increase in intestinal permeability in Caco-2 cells^[1].
In Vivo: Tegoprazan (30 mg / kg, p.o., twice daily for 5 days) alleviates the severity of dinitrobenzene sulfonic acid (DNBS)-induced reduced colon length and colonic damage, as well as protecting against DNBS-induced colon inflammation in mice colon^[1].
Tegoprazan (0.1, 1 and 10 mg/kg, p.o., a single day or daily for 5 days) exerts an antiulcer effect in Naproxen (HY-15030)-induced acute gastric ulcer rat model^[2].