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Description: Linaprazan (also known as AZD0865) is a novel, potent inhibitor of gastric H(+), K(+)-ATPase that inhibit acid formation in vitro with a fast onset of effect. AZD0865 belongs to a new class of acid-suppressing agents with rapid onset of action and potent acid inhibition. It inhibits gastric H(+), K(+)-ATPase by K(+)-competitive binding. In porcine ion-leaky vesicles at pH 7.4, AZD0865 concentration-dependently inhibited K(+)-stimulated H(+), K(+)-ATPase activity (IC(50) 1.0+/-0.2 microM) but was more potent at pH 6.4 (IC(50) 0.13+/-0.01 microM).
References: Biochem Pharmacol. 2007 Jan 15; 73(2):198-205.; Clin Gastroenterol Hepatol. 2007 Dec; 5(12):1385-91.
Related CAS: 248919-64-4; 855998-67-3 (mesylate)
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