942195-55-3

942195-55-3 structure

Name: Tegoprazan
Chemical Name: Tegoprazan
CAS Number: 942195-55-3
Molecular Formula: C₂₀H₁₉F₂N₃O₃
Molecular Weight: 387.38
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Proton Pump
Create Date: 2019-02-16 15:53:47
Modify Date: 2024-01-05 10:26:41
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].

Name	Tegoprazan

Description	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].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Proton Pump Research Areas >> Metabolic Disease
Target	IC50: 0.29-0.52 μM (H+/K+-ATPase)[1].
In Vitro	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].
In Vivo	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].
References	[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.