Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE2-PCCAhydrochlorideCat.No.:HY-100013C分?式:C??H??ClN?O分?量:492.1作?靶點:GPR88作?通路:GPCR/GProtein儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數據體外實驗DMSO:100mg/mL(203.21mM;Needultrasonic)H2O:20mg/mL(40.64mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0321mL10.1605mL20.3211mL5mM0.4064mL2.0321mL4.0642mL10mM0.2032mL1.0161mL2.0321mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.08mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.08mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.08mM);ClearsolutionBIOLOGICALACTIVITY?物活性2-PCCAhydrochloride?種外消旋體，為GPR88受體激動劑，在HEK293細胞中，可抑制GPR88介導的cAMP的產?，EC50值為116nM。IC50&TargetEC50:116nM(GPR88receptor,HEK293cells)[1]體外研究2-PCCAhydrochlorideinhibitsGPR88-mediatedcAMPproductionthroughaGαi-coupledpathway,withanEC50of116nMinHEK293cellsstablyexpressingthehumanGPR88receptorandtheGloSensor-22FcAMPconstruct[2].體內研究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