Endomorphin-1-acetate-DataSheet-生命科学试剂-MCEVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEndomorphin1acetateCat.No.:HY-P0185ACASNo.:1276123-71-7分⼦式:C₃₆H₄₂N₆O₇分⼦量:670.75作⽤靶点:OpioidReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:polypeptide,sealedstorage,awayfrommoistureandlight,undernitrogen*Insolvent:-80°C,6months;-20°C,1month(polypeptide,

sealedstorage,awayfrommoistureandlight,undernitrogen)溶解性数据体外实验DMSO:125mg/mL(186.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.4909mL7.4543mL14.9087mL5mM0.2982mL1.4909mL2.9817mL10mM0.1491mL0.7454mL1.4909mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight,undernitrogen)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.10mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.10mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.10mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Endomorphin1acetate，⼀种⾼度选择性的，⾼亲和⼒的μ-opioid受体激动剂(Ki:1.11nM)，对kappa3结合位点具有⾼亲和⼒，Ki值为20到30nM之间。Endomorphin1acetate具有镇痛特性。IC50&TargetμOpioidReceptor/MOR1.11nM(Ki)体外研究Endomorphin1acetateinhibitsForskolin(HY-15371)(1μM)stimulatedcyclicAMPformationwithapIC50valueof8.03inInCHOμcells[5].Endomorphin1(1-10μM)acetateincreasesinterleukin-8secretioninCaco-2cells[6].Endomorphin1(1μM)acetateinhibitsexcitatorytransmissioninadultratsubstantiagelatinosaneurons[7].体内研究Endomorphin1(i.c.v.)acetateshowsantinociceptivepropertiesinmice,withanED50valueof6.16nM[2].Endomorphin1(50μg/kg,i.v.,rats)acetatealleviatesmyocardialischemia/reperfusioninjury(MIRI)byinhibitingtheinflammatoryresponse[3].AnimalModel:ICRmice[2].Dosage:6.16nM(ED50)Administration:Intracerebroventricularly(i.c.v.)injectionResult:Inhibiteddose-dependentlythetail-flickresponse.AnimalModel:Rats[3].Dosage:50μg/kgAdministration:IntravenouslyfollowingLADligationfor25min,subsequentlytheLADwasreperfusedfor120min.Result:AlleviatedMIRIbyreducingtheproductionoffreeradicals.DncreasedLDHandCK-MBactivities.IncreasedSODactivityanddecreasedMDAcontent.DecreasedIL-6andTNF-αplasmacontent.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].GoldbergIE,etal.Pharmacologicalcharacterizationofendomorphin-1andendomorphin-2inmousebrain.JPharmacolExpTher.1998Aug;286(2):1007-13.[2].TsengLF.Theantinociceptivepropertiesofendomorphin-1andendomorphin-2inthemouse.JpnJPharmacol.2002Jul;89(3):216-20.[3].ZhangWP,etal.Effectsofendomorphin-1postconditioningonmyocardialischemia/reperfusioninjuryandmyocardialcellapoptosisinaratmodel.MolMedRep.2016Oct;14(4):3992-8.[4].KodaY,etal.Synthesisandinvitroevaluationofalibraryofmodifiedendomorphin1peptides.BioorgMedChem.2008Jun1;16(11):6286-96.[5].HarrisonC,etal.Theeffectsofendomorphin-1andendomorphin-2inCHOcellsexpressingrecombinantmu-opioidreceptorsandSH-SY5Ycells.BrJPharmacol.1999Sep;128(2):472-8.[6].NeudeckBL,etal.Endomorphin-1altersinterleukin-8secretioninCaco-2cellsviaareceptormediatedprocess.ImmunolLett.2002Dec3;84(3):217-21.[7].FujitaT,etal.Inhibitionbyendomorphin-1andendomorphin-2ofexcitatorytransmissioninadultratsubstantiagelatinosaneurons.Neuroscience.2006;139(3):1095-105.McePdfHeightCaut