Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE(1R,2R)-2-PCCAhydrochlorideCat.No.:HY-100013A1CASNo.:1609563-71-4分?式:C??H??Cl?N?O分?量:528.56作?靶點(diǎn):GPR88作?通路:GPCR/GProtein儲(chǔ)存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(94.60mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8919mL9.4597mL18.9193mL5mM0.3784mL1.8919mL3.7839mL10mM0.1892mL0.9460mL1.8919mL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(storedundernitrogen)。-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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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(4.73mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.73mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性(1R,2R)-2-PCCAhydrochloride?種有效的GPR88受體激動(dòng)劑，?細(xì)胞體系下，EC50值為3nM，細(xì)胞體系下EC50值為603nM。IC50&TargetEC50:3nM(GPR88receptor)[1],603nM(GPR88receptor,inGPR88-22Fcells)[2]體外研究(1R,2R)-2-PCCA(Example3)isapotentGPR88receptoragonist,withanEC50of3nMincell-freeassay,and603nMincellassay[1][2].(1R,2R)-2-PCCAinhibitsGPR88-mediatedcAMPproductionthroughaGαi-coupledpathway,withanEC50of56nMinHEK293cellsstablyexpressingthehumanGPR88receptorandtheGloSensor-22FcAMPconstruct[2].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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