Tegoprazan

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型强效、高选择性、竞争性和口服活性的胃 H+/K+-ATP 酶抑制剂，体外猪、犬和人 H+/K+-ATP 酶的 IC50 范围为 0.29-0.52 uM。

A novel potent, highly selective, competitive and orally active inhibitor of gastric H+/K+-ATPase with IC50 of ranging 0.29-0.52 uM porcine, canine and human H+/K+-ATPases in vitro; displays no activity against canine kidney Na+/K+-ATPase (IC50>100 uM); potently inhibits histamine-induced gastric acid secretion in dogs and a complete inhibition at 1.0 mg/kg starting from 1 hr after administration, reverses the pentagastrin-induced acidified gastric pH to the neutral range at 1-3 mg/kg, immediately evoks a gastric phase III contraction of migrating motor complex (MMC) in pentagastrin-treated dogs.Ulcer Phase 3 Clinical(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.(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.

——

——

CJ 12420 | RQ-00000004 | RQ-4

Membrane Transporter/Ion Channel

Proton Pump

Proton Pump

Other Indications

Ulcer

942195-55-3

387.387

C20H19F2N3O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (258.14 mM)

O=C(C1=CC(O[C@H]2CCOC3=C2C(F)=CC(F)=C3)=C4C(NC(C)=N4)=C1)N(C)C

(S)-4-((5,7-difluorochroman-4-yl)oxy)-N,N,2-trimethyl-1H-benzo[d]imidazole-6-carboxamide

(-20℃)

With Ice Pack

≥ 2 years