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Lansoprazole(AG 1749)
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。
Lansoprazole(AG 1749)图片
CAS NO:103577-45-3
规格:≥98%
包装与价格:
包装价格(元)
250mg询价
500mg询价
1g询价
2g询价
5g询价
10g询价

Lansoprazole (formerly A65006, AG1749; A-65006, AG-1749; trade name Prevacid, Zoton, Agopton, Bamalite, Opiren), a prescription and OTC drug for treatment for heartburn, is a potent and next generation proton-pump inhibitor (PPI) which prevents the stomach from producing gastric acid. Lansoprazole has the same pharmacologic class as omeprazole which inhibits the stomach's production of gastric acids. Research is underway for analogs of lansoprazole to explore their use as potential PET imaging agents for diagnosing tauopathies including Alzheimer's disease. Lansoprazole is also a prodrug that targets the cytochrome bc1 complex of Mycobacterium tuberculosis once converted to lansoprazole sulfide in mycobacterial host cells.
理化性质和储存条件
Molecular Weight (MW)369.36
FormulaC16H14F3N3O2S
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)

Chemical Name: 2-[[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl]-1H-benzimidazole

InChi Key: MJIHNNLFOKEZEW-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H14F3N3O2S/c1-10-13(20-7-6-14(10)24-9-16(17,18)19)8-25(23)15-21-11-4-2-3-5-12(11)22-15/h2-7H,8-9H2,1H3,(H,21,22)

SMILES Code: O=S(C1=NC2=CC=CC=C2N1)CC3=NC=CC(OCC(F)(F)F)=C3C

SynonymsA-65006, AG-1749; A65006, AG1749; A 65006, AG 1749; Prevacid, Zoton, Agopton, Bamalite, Opiren
实验参考方法
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.

In VivoLansoprazole 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 modelRats
Formulation & Dosage
References

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

 
 
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