Tegoprazan 是一种口服有效的、高选择性胃H+/K+-ATP酶 (H+/K+-ATPase) 抑制剂，能够控制胃酸分泌和运动，在体外检测的对猪、犬、人的H+/K+-ATP酶的IC50为0.29-0.52 μM。

Tegoprazan is a potassium-competitive acid blocker and is a potent, oral active, and highly selective inhibitor of gastric H+/K+-ATPase. That could control gastric acid secretion and motility (IC50: ranging from 0.29-0.52 μM for porcine, canine, and human H+/K+-ATPases in vitro).

Tegoprazan inhibits gastric H+/K+-ATPase in a potassium-competitive and reversible manner and it also inhibits porcine, canine, and human H+/K+-ATPase activity. Tegoprazan (3 μM) inhibits 86% of H+/K+-ATPase activity, whereas the inhibition is decreased to 34% after the dilution of Tegoprazan concentration to 0.15 μM [1].

Tegoprazan (1.0-3.0 mg/kg, p.o.) reverses the pentagastrin-induced acidified gastric pH to the neutral range. Tegoprazan (1.0 mg/kg, p.o.) effectively and fully inhibits histamine-induced gastric acid secretion in dogs. Tegoprazan (3 mg/kg, p.o.) immediately evokes a gastric phase III contraction of the migrating motor complex in pentagastrin-treated dogs [1].

942195-55-3

C20H19F2N3O3

387.38

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