Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESEN12333Cat.No.:HY-107678CASNo.:874450-44-9Synonyms:WAY-317538分?式:C??H??N?O?分?量:339.43作?靶點:nAChR作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(294.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9461mL14.7306mL29.4612mL5mM0.5892mL2.9461mL5.8922mL10mM0.2946mL1.4731mL2.9461mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)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(xiàn)沉淀、析出現(xiàn)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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(7.37mM);ClearsolutionBIOLOGICALACTIVITY?物活性SEN12333?種強效、選擇性和?服活性的α7nAChR激動劑。SEN12333對GH4C1細胞中表達的??α7nAChRs具有很?的親和性(K>i=260nM)，并在功能性Ca2+通量研究(EC50=1.6μM)中起到完全激動劑的作?。SEN12333可以?于AD和精神分裂癥研究。體外研究Inwhole-cellpatch-clamprecordings,SEN12333activatespeakcurrentsandmaximaltotalchargessimilartoacetylcholine(EC50=12μM).SEN12333displaysfunctionalantagonismathistamineH3receptors(IC50=103nM)andweakagonistactivityathumanganglionicα3nAChRs(IC50=8.5μM)[1].體內(nèi)研究SEN12333(intraperitonealinjection;3mg/kg)improvesepisodicmemoryinanovelobjectrecognitiontaskinratsinconditionsofspontaneousforgettingaswellascognitivedisruptionsinducedviaglutamatergicorcholinergicmechanisms.SEN12333alsopreventsascopolamine-induceddeficitinapassiveavoidancetask[1].REFERENCES[1].CorinneBeinat,etal.TheRecentDevelopmentofα7NicotinicAcetylcholineReceptor(nAChR)LigandsasTherapeuticCandidatesfortheTreatmentofCentralNervousSystem(CNS)Diseases.CurrPharmDes.2016;22(14):2134-51.[2].RenzaRoncarati,etal.Procognitiveandneuroprotectiveactivityofanovelalpha7nicotinicacetylcholinereceptoragonistfortreatmentofneurodegenerativeandcognitivedisorders.JPharmacolExpTher.2009May;329(2):459-68.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch