Exendin-4-Exenatide-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEExendin-4Cat.No.:HY-13443CASNo.:141758-74-9Synonyms:Exenatide分⼦式:C₁₈₄H₂₈₂N₅₀O₆₀S分⼦量:4186.57Sequence:His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-

Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2SequenceShortening:HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2作⽤靶点:GCGR作⽤通路:GPCR/GProtein储存⽅式:ProtectfromlightPowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY⽣物活性Exendin-4(Exenatide)由39个氨酸组成的多肽。它长效的glucagon-likepeptide-1受体激动剂，IC50值为3.22nM。IC50&TargetIC50:3.22nM(glucagon-likepeptide-1receptor)[1]体外研究Inhumanumbilicalveinendothelialcells,exendin-4significantlyincreasesNOproduction,endothelialNOsynthase(eNOS)phosphorylation,andGTPcyclohydrolase1(GTPCH1)levelinadose-dependentmanner[2].Exendin-4showscytotoxiceffectstoMCF-7breastcancercellswithIC50of5μMat48hour[3].体内研究Bothlow-andhigh-doseexendin-4treatmentinob/obmiceimproveserumALTandreduceserumglucose,andcalculatedHOMAscorescomparedwithcontrol.Exendin-4-treatedob/obmicesustainamarkedreductioninthenetweightgaininthefinal4weeksofthestudyperiod[4].Animalstreatedwithexendin-4havemorepancreaticacinarinflammation,morepyknoticnucleiandweighsignificantlylessthancontrolrats.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEExendin-4treatmentisassociatedwithlowerleptinlevelsaswellaslowerHOMAvaluesinrats[5].Exenatidecausesdose-dependentrelaxationofratthoracicaorta,whichisevokedviatheGLP-1receptorandismediatedmainlybyH2SbutalsobyNOandCO[6].PROTOCOLAnimalRats:20Sprague-Dawleymalerats,tenofwhicharetreatedwithexendin-4(10μg/kg)andtenofwhichareAdministration[4][5]usedascontrols.Thestudyperiodis75days.Serumandpancreatictissueareremovedforbiochemicalandhistologicalstudy.Bloodglucose,amylase,lipaseandadipocytokinesarecomparedbetweenthetwogroups[5].Mice: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.户使⽤本产品发表的科研⽂献•Gut.2022Jun13;gutjnl-2021-326541.•Biomaterials.2021Aug;275:120944.•IntJBiolSci.2022;18(4):1328-1346.•JNeuroinflammation.2019Nov28;16(1):242.•BrJPharmacol.2020Aug;177(15):3389-3402.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DoyleME,etal.Theimportanceofthenine-aminoacidC-terminalsequenceofexendin-4forbindingtotheGLP-1receptorandforbiologicalactivity.RegulPept.2003Jul15;114(2-3):153-8.[2].WeiR,etal.ExenatideexertsdirectprotectiveeffectsonendothelialcellsthroughtheAMPK/Akt/eNOSpathwayinaGLP-1receptor-dependentmanner.AmJPhysiolEndocrinolMetab.2016Jun1;310(11):E947-57.[3].Fidan-YaylalIG,etal.Antidiabeticexendin-4activatesapoptoticpathwayandinhibitsgrowthofbreastcancercells.TumourBiol.2016Feb;37(2):2647-53.[4].DingX,etal.Exendin-4,aglucagon-likeprotein-1(GLP-1)receptoragonist,reverseshepaticsteatosisinob/obmice.Hepatology.2006Jan;43(1):173-81.[5].NachnaniJS,etal.Biochemicalandhistologicaleffectsofexendin-4(exenatide)ontheratpancreas.Diabetologia.2010Jan;53(1):153-9.[6].SelleyE,etal.Exenatideinducesaorticvasodilationincreasinghydrogensulphide,carbonmonoxideandnitricoxideproduction.CardiovascDiabetol.2014Apr2;13:69.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www