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AZD0865

Names

[ CAS No. ]:
248919-64-4

[ Name ]:
AZD0865

[Synonym ]:
Linaprazan [INN:BAN]
UNII-E0OU4SC8DP
AZD0865
Linaprazan

Biological Activity

[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.


[Related Small Molecules]

Bafilomycin A1 | omeprazole | Vonoprazan Fumarate (TAK-438) | Zinc Pyrithione | Lansoprazole | Ilaprazole | Soraprazan | bamaquimast | Esomeprazole | Esomeprazole magnesium | Chebulinic acid | Picoprazole | SKF96067 | Pumaprazole | S3337

Chemical & Physical Properties

[ Molecular Formula ]:
C21H26N4O2

[ Molecular Weight ]:
366.45700

[ Exact Mass ]:
366.20600

[ PSA ]:
82.15000

[ LogP ]:
3.54990


Related Compounds

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