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product name Lansoprazole


Description: Lansoprazole (also known as A-65006, AG-1749) is a potent proton-pump inhibitor (PPI) which prevents the stomach from producing gastric acid. Lansoprazole has the same pharmacologic class as omeprazole which inhibits the stomachs production of gastric acids. Research is underway for analogs of lansoprazole to explore their use as potential PET imaging agents for diagnosing tauopathies including Alzheimers disease. Lansoprazole is also a prodrug that targets the cytochrome bc1 complex of Mycobacterium tuberculosis once converted to lansoprazole sulfide in mycobacterial host cells. 

References: Ann Pharmacother. 1996 Dec;30(12):1425-36; J Clin Biochem Nutr. 2009 Jul;45(1):9-13. 



Molecular Weight (MW)

369.36
Formula

C16H14F3N3O2
CAS No.

103577-45-3
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 74 mg/mL (200.3 mM)
Water: <1 mg/mL
Ethanol: 14 mg/mL (37.9 mM)
Solubility (In vivo)

 
Synonyms

A-65006, AG-1749

other peoduct :

In Vitro

In vitro activity: Lansoprazole inhibits gastric acid secretion via inhibition of gastric hydrogen/potassium adenosine triphosphatase (H+,K(+)-ATPase), an enzyme of the gastric parietal cell membrane that forms part of the proton pump that performs the final step in the acid secretory process. Lansoprazole binds covalently to parietal cell H+,K(+)-ATPase, rendering it nonfunctional and inhibiting the secretion of gastric acid. Lansoprazole is a strong anti-secretory agent that acts on gastric H+/K+-adenosine triphosphatase (H+/K+ ATPase) of parietal cells. Lansoprazole inhibits the increased expression of vascular adhesion molecules, the activation of neutrophils, and the production of pro-inflammatory cytokines from activated endothelial cells. Lansoprazole induces several genes, including phase II detoxifying enzyme (NADPH-ubiquinone oxidoreductase, glutathione S-transferase) and antioxidant stress proteins (HO-1, thioredoxin reductase, and superoxide dismutase) in gastric epithelial cells. Lansoprazole significantly inhibits the production of CINC-1 from stimulated RGM-1 cells with IL-1β. Lansoprazole up-regulates HO-1 expression throughout Nrf2 in rat gastric epithelial cells, and the up-regulated HO-1 has anti-inflammatory effects.


Kinase Assay


Cell Assay

In Vivo Lansoprazole inhibits acute inflammatory reactions as well as intestinal mucosal injuries induced by ischemia-reperfusion or indomethacin administration in rats. Lansoprazole significantly inhibits intestinal injuries induced by ischemia-reperfusion or indomethacin. lansoprazole administered exogenously prevents the small intestine against ischemia-reperfusion or indomethacin-induced damage, the action being dependent on its anti-inflammatory and anti-oxidative responses. 
Animal model  
Formulation & Dosage  
References Ann Pharmacother. 1996 Dec;30(12):1425-36; J Clin Biochem Nutr. 2009 Jul;45(1):9-13. 

THZ4 (Hydrochloride)

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Author: Sodium channel