Linaprazan (AZD0865) (Synonyms: Linaprazan) |
| رقم الكتالوجGC32924 |
يثبط Linaprazan (AZD0865) (AZD0865) المعدة H+ ، K+-ATPase بواسطة K+- الربط التنافسي.
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Cas No.: 248919-64-4
Sample solution is provided at 25 µL, 10mM.
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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.
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