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Linaprazan(AZD0865)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Linaprazan(AZD0865)图片
CAS NO:248919-64-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Linaprazan (AZD0865) (AZD0865) 通过 K+- 竞争性结合抑制胃 H+,K+-ATPase。
Cas No.248919-64-4
别名利那拉生; AZD0865
Canonical SMILESO=C(C1=CN2C(C(NCC3=C(C)C=CC=C3C)=C1)=NC(C)=C2C)NCCO
分子式C21H26N4O2
分子量366.46
溶解度DMSO : ≥ 35 mg/mL (95.51 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.