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Medchemexpress/Exendin-4(同义词:艾塞那肽;他的Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln符合Glu-Glu-Glu-Ala-Val-Arg
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- •SciRep.2017Jun28;7(1):4351.
- •ActaBiochimBiophysSin(Shanghai).2017May5:1-8.
Description | Exendin-4,a39aminoacidpeptide,isalong-actingglucagon-likepeptide-1receptoragonistwithanIC50of3.22nM. |
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IC50&Target | IC50:3.22nM(glucagon-likepeptide-1receptor)[1] |
InVitro | Inhumanumbilicalveinendothelialcells,exendin-4significantlyincreasesNOproduction,endothelialNOsynthase(eNOS)phosphorylation,andGTPcyclohydrolase1(GTPCH1)levelinadose-dependentmanner[2].Exendin-4showscytotoxiceffectstoMCF-7breastcancercellswithIC50of5μMat48hour[3]. |
InVivo | Bothlow-andhigh-doseexendin-4treatmentinob/obmiceimproveserumALTandreduceserumglucose,insulinlevelsandcalculatedHOMAscorescomparedwithcontrol.Exendin-4-treatedob/obmicesustainamarkedreductioninthenetweightgaininthefinal4weeksofthestudyperiod[4].Animalstreatedwithexendin-4havemorepancreaticacinarinflammation,morepyknoticnucleiandweighsignificantlylessthancontrolrats.Exendin-4treatmentisassociatedwithlowerinsulinandleptinlevelsaswellaslowerHOMAvaluesinrats[5].Exenatidecausesdose-dependentrelaxationofratthoracicaorta,whichisevokedviatheGLP-1receptorandismediatedmainlybyH2SbutalsobyNOandCO[6]. |
ClinicalTrial | ViewMoreCollapse |
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AnimalAdministration [4][5] | Rat:20Sprague-Dawleymalerats,tenofwhicharetreatedwithexendin-4(10μg/kg)andtenofwhichareusedascontrols.Thestudyperiodis75days.Serumandpancreatictissueareremovedforbiochemicalandhistologicalstudy.Bloodglucose,amylase,lipase,insulinandADIpocytokinesarecomparedbetweenthetwogroups[5]. Mouse:Theexendin-4treatmentgroupsaretreatedwith10μg/kgevery24hoursforthefirst14days.Thistreatmentistheinductionphase.Respectivecontrolmice(leanandob/ob)receivesalineevery24hours.After14daysExendin-4-treatedmicearerandomlydividedintotwogroups:onegroupreceiveshighdoseexendin-4(20μg/kg)every12hours,whilethesecondgroupcontinueswithlowdoseexendin-4(10μg/kg)every12hours.Thecontrolmicecontinuetoreceivesalineevery12hours.Themiceareweigheddailyforthe60-daytreatmentperiod[4]. MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.References |
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