Linaprazan-mesylate-AZD-0865-mesylate-生命科学试剂-MCE.pdf

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Inhibitors•ScreeningLibraries•Proteins

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Linaprazanmesylate

Cat.No.:HY-100412A

CASNo.:855998-67-3

Synonyms:AZD-0865mesylate

分⼦式:C₂₂H₃₀N₄O₅S

分⼦量:462.56

作⽤靶点:ProtonPump

作⽤通路:MembraneTransporter/IonChannel

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性Linaprazan(AZD0865)mesylate能够通过K+竞争约束抑制胃⾥H+,K+-ATPase.(IC50:1.0±0.2μM)，它对

酸有很强的抑制作⽤。Linaprazan(AZD0865)mesylate可⽤于研究反流性⾷管炎，具有⼝服有效性。

体外研究Linaprazan(AZD0865)mesylateinhibitsacidformationinrabbitgastricglandsstimulatedbyhistamineor

dibutyrylcAMP(IC50valuesof0.28and0.26μM,respectively)[1].

Linaprazan(AZD0865)mesylate(3μM,pH7.4)inhibitsH+,K+-ATPaseactivityby88.1%[1].

Linaprazan(AZD0865)mesylateinhibitsH+,K+-ATPaseactivityinaK+-competitivemanner(Ki=46nM)[1].

体内研究

Pharmacokineticanalysisof2.4mg/kgLinaprazanmesylateaftersingleoraladministrationinSDrats[3]

Sext1/2(h)Tmax(h)Cmax(ngeq./g)AUC0-t(ng·heq./g)AUC0-∞(ng·heq./g)AUC%(%)

Male5.084.67455596062004.12Femal4.644.00127013900143003.10

REFERENCES

[1].GeddaKetal.MechanismofactionofAZD0865,aK+-compe