Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEndomorphin1acetateCat.No.:HY-P0185ACASNo.:1276123-71-7分?式:C??H??N?O?分?量:670.75作?靶點(diǎn):OpioidReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:polypeptide,sealedstorage,awayfrommoistureandlight,undernitrogen*Insolvent:-80°C,6months;-20°C,1month(polypeptide,

sealedstorage,awayfrommoistureandlight,undernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(186.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.4909mL7.4543mL14.9087mL5mM0.2982mL1.4909mL2.9817mL10mM0.1491mL0.7454mL1.4909mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight,undernitrogen)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.10mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.10mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.10mM);ClearsolutionBIOLOGICALACTIVITY?物活性Endomorphin1acetate，?種?度選擇性的，?親和?的μ-opioid受體激動(dòng)劑(Ki:1.11nM)，對(duì)kappa3結(jié)合位點(diǎn)具有?親和?，Ki值為20到30nM之間。Endomorphin1acetate具有鎮(zhèn)痛特性。IC50&TargetμOpioidReceptor/MOR1.11nM(Ki)體外研究Endomorphin1acetateinhibitsForskolin(HY-15371)(1μM)stimulatedcyclicAMPformationwithapIC50valueof8.03inInCHOμcells[5].Endomorphin1(1-10μM)acetateincreasesinterleukin-8secretioninCaco-2cells[6].Endomorphin1(1μM)acetateinhibitsexcitatorytransmissioninadultratsubstantiagelatinosaneurons[7].體內(nèi)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?邊的抑制劑?師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