Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEExendin-4Cat.No.:HY-13443CASNo.:141758-74-9分?式:C???H???N??O??S分?量:4186.57Sequence:His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-A

la-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-

Pro-Pro-Pro-Ser-NH2SequenceHGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2Shortening:作?靶點:GlucagonReceptor作?通路:GPCR/GProtein儲存?式:ProtectfromlightPowder-80°C2years-20°C1year*Insolvent:-80°C,6months;-20°C,1month(protectfromlight)溶解性數據體外實驗H2O:≥50mg/mL(11.94mM)掃描?維碼，DMSO:≥32mg/mL(7.64mM)運?溶解?案計算器*"≥"meanssoluble,butsaturationunknown.獲得適合您實驗體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM0.2389mL1.1943mL2.3886mL5mM0.0478mL0.2389mL0.4777mL10mM0.0239mL0.1194mL0.2389mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的?式助溶1/4www.MedChemEwww.MedChemE1.請依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.5mg/mL(0.60mM);Clearsolution此?案可獲得≥2.5mg/mL(0.60mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述2.體系中加?50μLTween-80，混合均勻；然后繼續加?450μL?理鹽?定容?1mL。請依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(0.60mM);Clearsolution此?案可獲得≥2.5mg/mL(0.60mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.5mg/mL(0.60mM);Clearsolution此?案可獲得≥2.5mg/mL(0.60mM，飽和度未知)的澄溶液，此?案不適?于實驗周期在半個?以上的實驗。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性Exendin-4(Exenatide)由39個氨酸組成的多肽。它長效的glucagon-likepeptide-1受體激動劑，IC50值為3.22nM。IC50&TargetIC50:3.22nM(glucagon-likepeptide-1receptor)[1]體外研究Inhumanumbilicalveinendothelialcells,exendin-4significantlyincreasesNOproduction,endothelialNOsynthase(eNOS)phosphorylation,andGTPcyclohydrolase1(GTPCH1)levelinadose-dependentmanner[2].Exendin-4showscytotoxiceffectstoMCF-7breastcancercellswithIC50of5μMat48hour[3].體內研究Bothlow-andhigh-doseexendin-4treatmentinob/obmiceimproveserumALTandreduceserumglucose,andcalculatedHOMAscorescomparedwithcontrol.Exendin-4-treatedob/obmicesustainamarkedreductioninthenetweightgaininthefinal4weeksofthestudyperiod[4].Animalstreatedwithexendin-4havemorepancreaticacinarinflammation,morepyknoticnucleiandweighsignificantlylessthancontrolrats.Exendin-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.2/4www.MedChemEwww.MedChemEAfter14daysExendin-4-treatedmicearerandomlydividedintotwogroups:onegroupreceiveshighdoseexendin-4(20μg/kg)every12hours,whilethesecondgroupcontinueswithlowdoseexendin-4(10μg/kg)every12hours.Thecontrolmicecontinuetoreceivesalineevery12hours.Themiceareweigheddailyforthe60-daytreatmentperiod[4].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產品發表的科研?獻?BrJPharmacol.2020Aug;177(15):3389-3402.?BMCBiol.2021Mar3;19(1):40.?JNeuroinflammation.2019Nov28;16(1):242.?JCellPhysiol.2021May;236(5):3641-3659.?Biomedicines.2020Nov9;8(11):E485.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.McePdfHeight3/4www.MedChemEwww.Me