Tegoprazan是钾竞争性酸阻滞剂，是有效的、有口服活性的、高度选择性的胃H+/K+-ATP酶(H+/K+-ATPase)的抑制剂，能够控制胃酸分泌和运动，其在体外检测的对猪、犬、人的H+/K+-ATP酶的IC50值为0.29-0.52μM。
货号:ajcx12606
CAS:942195-55-3
分子式:C20H19F2N3O3
分子量：387.38
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Tegoprazan, a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H+/K+-ATPases in vitro[1].

Tegoprazan inhibits porcine, canine, and human H+/K+-ATPase activity. Tegoprazan inhibits gastric H+/K+-ATPase in a potassium-competitive and reversible manner. 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 mg/kg, p.o.) potently and completely inhibits histamine-induced gastric acid secretion in dogs. Tegoprazan (1.0-3.0 mg/kg, p.o.) reverses the pentagastrin-induced acidified gastric pH to the neutral range. Tegoprazan (3 mg/kg, p.o.) immediately evokes a gastric phase III contraction of the migrating motor complex in pentagastrin-treated dogs[1].

[1]. Takahashi N, et al. Tegoprazan, a Novel Potassium-Competitive Acid Blocker to Control Gastric Acid Secretion and Motility. J Pharmacol Exp Ther. 2018 Feb;364(2):275-286.