248919-64-4

248919-64-4 structure

Name: AZD0865
Chemical Name: 8-[(2,6-dimethylphenyl)methylamino]-N-(2-hydroxyethyl)-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide
CAS Number: 248919-64-4
Molecular Formula: C₂₁H₂₆N₄O₂
Molecular Weight: 366.45700
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Proton Pump
Create Date: 2018-10-13 18:04:23
Modify Date: 2024-01-04 15:55:55
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.

Name	8-[(2,6-dimethylphenyl)methylamino]-N-(2-hydroxyethyl)-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide
Synonyms	Linaprazan [INN:BAN] UNII-E0OU4SC8DP AZD0865 Linaprazan

Description	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.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Proton Pump Research Areas >> Cancer
References	[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.