GZR18--生命科学试剂-MCE.pdf

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Inhibitors•ScreeningLibraries•Proteins

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GZR18

Cat.No.:HY-P10269

分⼦式:C₁₈₉H₂₉₅N₄₅O₅₉

分⼦量:4141.63

Sequence:His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Gl

u-Gly-Gln-Ala-Ala-Lys(Ala-Glu-Glu-Ala-Ala-Glu-Glu-Ala-gamm

aGlu-C22diacid)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly

SequenceShortening:HGEGTFTSDVSSYLEGQAA-K(AEEA-AEEA-gammaGlu-C22

diacid)-EFIAWLVRGRG

作⽤靶点:GLPReceptor

作⽤通路:GPCR/GProtein

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性GZR18是胰⾼⾎糖素样肽-1(GLP-1)的类似物，对GLP-1受体具有激动活性，EC50为0.677nM。GZR18可以

减轻2型糖尿病[1]。

IC50TargetEC50:0.677nM(GLP-1Receptor)

体外研究GZR18(30-90nM,0.5-1h)stimulatesglucose-dependentinsulinsecretioninmousepancreaticisletβ-cells

inadose-dependentmanner[1].

体内研究GZR18(0-100nmol/kg,s.c.,singledoseor11dosages)decreasesbloodglucoselevelsandbodyweight

dose-depedently,andexhibitsglycemiccontrolpropertyindb/dbmicemodel[1].

GZR18(60μg/kg,ivorsc,singledose)revealsapharmacokineticprofilincynomolgusmonkeymodel[1].

PharmacokineticAnalysisofG