SEN12333-WAY-317538-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESEN12333Cat.No.:HY-107678CASNo.:874450-44-9Synonyms:WAY-317538分⼦式:C₂₀H₂₅N₃O₂分⼦量:339.43作⽤靶点:nAChR作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(294.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9461mL14.7306mL29.4612mL5mM0.5892mL2.9461mL5.8922mL10mM0.2946mL1.4731mL2.9461mL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。-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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(7.37mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性SEN12333⼀种强效、选择性和⼝服活性的α7nAChR激动剂。SEN12333对GH4C1细胞中表达的⼤⿏α7nAChRs具有很⾼的亲和性(K>i=260nM)，并在功能性Ca2+通量研究(EC50=1.6μM)中起到完全激动剂的作⽤。SEN12333可以⽤于AD和精神分裂症研究。体外研究Inwhole-cellpatch-clamprecordings,SEN12333activatespeakcurrentsandmaximaltotalchargessimilartoacetylcholine(EC50=12μM).SEN12333displaysfunctionalantagonismathistamineH3receptors(IC50=103nM)andweakagonistactivityathumanganglionicα3nAChRs(IC50=8.5μM)[1].体内研究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