AZD0865能够通过K+竞争约束抑制胃里H+,K+-ATPase.(IC50:1.0±0.2μM)，它对酸有很强的抑制作用。
CAS：248919-64-4
分子式：C21H26N4O2
分子量：366.46
纯度：98%
存储：Store at -20°C

Background:

AZD0865 inhibits gastric H+,K+-ATPase by K+-competitive binding. (IC50: 1.0 ± 0.2 μM)It is a acid-suppressing agents with rapid onset of action and potent acid inhibition. In vitro: AZD0865 can inhibit the final step in acid secretion. AZD0865 reduced porcine renal Na+,K+-ATPase activity by 9 ± 2%, demonstrating a high selectivity for H+,K+-ATPase.In vivo: The reference for animal administration is 0.5-1.0 mg/kg. The greater degree of acid suppression with the 75-mg dose of AZD0865 would translate to a healing rate of 89% at 4 weeks.

[1]. Gedda K et al. Mechanism of action of AZD0865, a K+-competitive inhibitor of gastric H+,K+-ATPase.Biochem Pharmacol. 2007 Jan 15;73(2):198-205. [2]. Kahrilas PJ et al. A randomized, comparative study of three doses of AZD0865 and esomeprazole for healing of reflux esophagitis. Clin Gastroenterol Hepatol. 2007 Dec;5(12):1385-91.