2-PCCA-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

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

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(203.21mM;Needultrasonic)H2O:20mg/mL(40.64mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0321mL10.1605mL20.3211mL5mM0.4064mL2.0321mL4.0642mL10mM0.2032mL1.0161mL2.0321mL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,awayfrommoisture)。-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:≥2.5mg/mL(5.08mM);Clearsolution2.請(qǐng)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(qǐng)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(dòng)劑，在HEK293細(xì)胞中，可抑制GPR88介導(dǎo)的cAMP的產(chǎn)?，EC50值為116nM。IC50&TargetEC50:116nM(GPR88receptor,HEK293cells)[1]體外研究2-PCCAhydrochlorideinhibitsGPR88-mediatedcAMPproductionthroughaGαi-coupledpathway,withanEC50of116nMinHEK293cellsstablyexpressingthehumanGPR88receptorandtheGloSensor-22FcAMPconstruct[2].體內(nèi)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