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

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE2-PCCAhydrochlorideCat.No.:HY-100013C分⼦式:C₃₀H₃₈ClN₃O分⼦量:492.1作⽤靶点:GPR88作⽤通路:GPCR/GProtein储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:100mg/mL(203.21mM;Needultrasonic)H2O:20mg/mL(40.64mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0321mL10.1605mL20.3211mL5mM0.4064mL2.0321mL4.0642mL10mM0.2032mL1.0161mL2.0321mL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,awayfrommoisture)。-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(5.08mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.08mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.08mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性2-PCCAhydrochloride⼀种外消旋体，为GPR88受体激动剂，在HEK293细胞中，可抑制GPR88介导的cAMP的产⽣，EC50值为116nM。IC50&TargetEC50:116nM(GPR88receptor,HEK293cells)[1]体外研究2-PCCAhydrochlorideinhibitsGPR88-mediatedcAMPproductionthroughaGαi-coupledpathway,withanEC50of116nMinHEK293cellsstablyexpressingthehumanGPR88receptorandtheGloSensor-22FcAMPconstruct[2].体内研究2-PCCA(0.1-3.2mg/kg,i.p.)decreasesthelocomotoractivityinratsinadose-dependentmannerinrats.2-PCCAcombinedwith1.0mg/kgmethamphetaminealsodose-dependentlyreducesmethamphetamine-inducedhyperactivity.2-PCCA(1-3.2mg/kg,i.p.)alonedoesnotproducemethamphetamine-likediscriminativestimuluseffects,oralterthediscriminativestimuluseffectsofmethamphetamine,whenstudiedincombination[1].PROTOCOLAnimalRats[1]Administration[1]Forthelocomotoractivitytests,ratsareonlyusedonce.Thetestisconductedinanadjacentroomfromtheanimalcolonyroomwithsimilarenvironmentalconditions(light,temperatureandhumidity).Beforetestsbegin,ratsareexposedtoatleastthreedaysofhandlingbytheexperimenter.Whenonly2-PCCA(1.0and3.2mg/kg)isstudied,thedrugis(i.p.)injectedimmediatelybeforetheratsareputintothetestchambersandthelocomotoractivityissimultaneouslyrecordedfor60min.When2-PCCAisstudiedincombinationwithmethamphetamine,thelocomotoractivityisrecordedfor20minandthenbothdrugsaresimultaneouslyinjectedandthelocomotoractivityisrecordedfor120moremin[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].LiJX,etal.TheGPR88receptoragonist2-PCCAdoesnotalterthebehavioraleffectsofmethamphetamineinrats.EurJPharmacol.2013Jan5;698(1-3):272-7.[2].JinC,etal.EffectofSubstitutionontheAnilineMoietyoftheGPR88Agonist2-PCCA:Synthesis,Structure-ActivityRelationships,andMolecularModelingStudies.ACSChemNeurosci.2016Oct19;7(10):1418-1432.McePdfHeightCaution:Producthasnotbeenfu