Tegoprazan (Synonyms: CJ-12420) |
Catalog No.GC31566 |
칼륨 경쟁적 산 차단제인 Tegoprazan은 위산 분비와 운동성을 조절할 수 있는 위산 H+/K+-ATPase의 강력한 경구 활성 및 고도 선택성 억제제이며 IC50 값 범위는 0.29-0.52입니다. 돼지, 송곳니 및 인간 H+/K+-ATPase의 시험관 내에서 μM.
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Cas No.: 942195-55-3
Sample solution is provided at 25 µL, 10mM.
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.
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