PZM21-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPZM21Cat.No.:HY-101386CASNo.:1997387-43-5分⼦式:C₁₉H₂₇N₃O₂S分⼦量:361.5作⽤靶点:OpioidReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(276.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7663mL13.8313mL27.6625mL5mM0.5533mL2.7663mL5.5325mL10mM0.2766mL1.3831mL2.7663mL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。-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:≥2.5mg/mL(6.92mM);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:≥2.5mg/mL(6.92mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.92mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PZM21⾼效选择性的μopioid受体激动剂，EC50值为1.8nM[1][2][3]。IC50&TargetEC50:1.8nM(μopioidreceptor)[1]体外研究PZM21hasnodetectableκORornociceptinreceptoragonistactivity-itisactuallyan18nMκORantagonist-whileitisa500-foldweakerδORagonist,makingitaselectiveμORagonist.AthERG,PZM21hasanIC50ofbetween2and4μM,500-to1,000-foldweakerthanitspotencyasaμORagonist.SignallingbyPZM21andotherμORagonistsappearstobemediatedprimarilybytheheterotrimericGproteinGi/o,asitseffectoncAMPlevelsiseliminatedbypertussistoxinandnoactivityisobservedinacalciumreleaseassay[1].体内研究PZM21isapotentGiactivatorwithexceptionalselectivityforμORandminimalβ-arrestin-2recruitment.PZM21isefficaciousfortheaffectivecomponentofanalgesiaversusthereflexivecomponentandisdevoidofrespiratorydepressioninmiceatequi-analgesicdoses.PZM21displaysdose-dependentanalgesiainamousehotplateassay,withapercentmaximalpossibleeffect(%MPE)of87%reached15minafteradministrationofthehighestdoseofdrugtested[1].PZM21hasalong-lastinganalgesiceffectonCNSmediated-painresponses,butdoesnotcauserespiratorydepressionandconstipation,twokeysideeffectsofopioidagonists[2].PROTOCOLAnimalMice:PZM21isdissolvedin0.9%sodiumchloride.MiceareinjectedwithPZM21(10mg/kg;20mg/kg;or40Administration[1]mg/kg).Afterinjectionofdrug,theanalgesiceffectexpressedaspercentagemaximumpossibleeffect(%MPE)ismeasuredat15,30,60,90and120minafterdrugtreatment[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Cell.2022Nov10;185(23):4361-4375.e19.•BrJPharmacol.2019Sep;176(17):3110-3125.•Neuroscience.2018Oct17;394:60-71.•Patent.US20220276244A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].ManglikA,etal.Structure-baseddiscoveryofopioidanalgesicswithreducedsideeffects.Nature.2016Sep8;537(7619):185-190.[2].KosticM,etal.BiasingOpioidReceptorsandCholesterolasaPlayerinDevelopmentalBiology.[3].AraldiD,etal.Mu-opioidReceptor(MOR)BiasedAgonistsInduceBiphasicDose-dependentHyperalgesiaandAnalgesia,andHyperalgesicPrimingintheRat.Neuroscience.2018Oct17;394:60-71.McePdfHeightCaution:Producth