SR-57227A-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESR57227ACat.No.:HY-102064CASNo.:77145-61-0分⼦式:C₁₀H₁₅Cl₂N₃分⼦量:248.15作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:8.33mg/mL(33.57mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.0298mL20.1491mL40.2982mL5mM0.8060mL4.0298mL8.0596mL10mM0.4030mL2.0149mL4.0298mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(8.38mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(8.38mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(8.38mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性SR57227A具有⼝服活性的5-HT3受体的⼀种选择性激动剂,可透过⾎脑屏障。SR57227A对⼤⿏⽪质膜和整个NG108-15细胞或其膜上5-HT3受体结合位点的亲和⼒(IC50)在2.8~250nM。具有抗抑郁作⽤。体外研究SR57227Abindsto5-HT3receptorslabelledwith[3H]S-zacopridewithanaffinity(Ki)of115nMinratcerebralcortex,150nMinNG108-15cellmembranesand103nMinwholeNG108-15cell[1].体内研究SR57227A(1-30mg/kg;i.p.)dose-dependentlyreducesimmobilitytimeintheforcedswimmingtestwithanED50valueforthiseffectof14.2mg/kg[2].Intheforcedswimmingtest,SR57227Adose-dependentlyreducesthedurationofimmobilityinratsafteri.p.administration.(ED50=7.6mg/kgi.p.inrats.)SR57227Aisalsoactiveinbothspeciesafteroraladministration.Inatime-coursestudyinmice,SR57227A(20mg/kgp.o.)producesasignificanteffectlasting6hours.SR57227A(1and3mg/kgi.p.)reducestheelevationoftheescapefailuresinthelearnedhelplessnessmodelinratsby50-60%onthelasttwodaysoftheavoidancetask,andreducesisolation-inducedaggressivityinmiceby50to85%,aneffectwhichisantagonisedbyZacopride(1mg/kgi.p.)[2].REFERENCES[1].PonceletM,etal,LeFurG.Antidepressant-likeeffectsofSR57227A,a5-HT3receptoragonist,inrodents.JNeuralTransmGenSect.1995;102(2):83‐90.[2].BachyA,etal.SR57227A:apotentandselectiveagonistatcentralandperipheral5-HT3receptorsinvitroandinvivo.EurJPharmacol.1993;237(2-3):299‐309.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicatio