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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Exendin-4(Synonyms: Exenatide; His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg
商品详细Medchemexpress/Exendin-4(Synonyms: Exenatide; His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg
Medchemexpress/Exendin-4(Synonyms: Exenatide; His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg
Medchemexpress/Exendin-4(Synonyms: Exenatide; His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg
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产品分类： 小分子
公司分类： Small_molecule
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商品介绍
Exendin-4,a39aminoacidpeptide,isalong-actingglucagon-likepeptide-1receptoragoNISTwithanIC50of3.22nM.

CustomerValidation

  • •SciRep.2017Jun28;7(1):4351.
  • •ActaBiochimBiophysSin(Shanghai).2017May5:1-8.
Description

Exendin-4,a39aminoacidpeptide,isalong-actingglucagon-likepeptide-1receptoragonistwithanIC50of3.22nM.

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
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References

  • [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-YaylalıG,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].SélleyE,etal.Exenatideinducesaorticvasodilationincreasinghydrogensulp,carbonmonoxideandnitricoxideproduction.CardiovascDiabetol.2014Apr2;13:69.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM0.2389mL1.1943mL2.3886mL
5mM0.0478mL0.2389mL0.4777mL
10mM0.0239mL0.1194mL0.2389mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
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

  • [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-YaylalıG,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].SélleyE,etal.Exenatideinducesaorticvasodilationincreasinghydrogensulp,carbonmonoxideandnitricoxideproduction.CardiovascDiabetol.2014Apr2;13:69.

MolecularWeight

4186.57

Formula

C₁₈₄H₂₈₂N₅₀O₆₀S

CASNo.

141758-74-9

Storage
Powder-80°C2years
 -20°C1year
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥32mg/mL;H2O:1.23mg/mL(Needultrasonicandwarming)

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:98.96%