1R-2R-2-PCCA-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE(1R,2R)-2-PCCAhydrochlorideCat.No.:HY-100013A1CASNo.:1609563-71-4分⼦式:C₃₀H₃₉Cl₂N₃O分⼦量:528.56作⽤靶点:GPR88作⽤通路:GPCR/GProtein储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:50mg/mL(94.60mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8919mL9.4597mL18.9193mL5mM0.3784mL1.8919mL3.7839mL10mM0.1892mL0.9460mL1.8919mL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(storedundernitrogen)。-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(4.73mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.73mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性(1R,2R)-2-PCCAhydrochloride⼀种有效的GPR88受体激动剂，⾮细胞体系下，EC50值为3nM，细胞体系下EC50值为603nM。IC50&TargetEC50:3nM(GPR88receptor)[1],603nM(GPR88receptor,inGPR88-22Fcells)[2]体外研究(1R,2R)-2-PCCA(Example3)isapotentGPR88receptoragonist,withanEC50of3nMincell-freeassay,and603nMincellassay[1][2].(1R,2R)-2-PCCAinhibitsGPR88-mediatedcAMPproductionthroughaGαi-coupledpathway,withanEC50of56nMinHEK293cellsstablyexpressingthehumanGPR88receptorandtheGloSensor-22FcAMPconstruct[2].户使⽤本产品发表的科研⽂献•NatCommun.2022May2;13(1):2375.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Bi,Yingzhi,etal.ModulatorsofGProtein-CoupledReceptor88.US20110251204A1.[2].JinC,etal.EffectofSubstitutionontheAnilineMoietyoftheGPR88Agonist2-PCCA:Synthesis,Structure-ActivityRelationships,andMolecularModelingStudies.ACSChemNeurosci.2016Oct19;7(10):1418-1432.[3].JinC,etal.Synthesis,pharmacologicalcharacterization,andstructure-activityrelationshipstudiesofsmallmolecularagonistsfortheorphanGPR88receptor.ACSChemNeurosci.2014Jul16;5(7):576-87.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc