Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESR142948TFACat.No.:HY-107664B分?式:C??H??F?N?O?分?量:799.88作?靶點(diǎn):NeurotensinReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性SR142948TFA?種具有?服活性、選擇性的?肽神經(jīng)降壓素受體(NT)拮抗劑，在h-NTR1-CHO細(xì)胞、HT-29細(xì)胞和成年??腦中的IC50分別為1.19nM、0.32nM、3.96nM。SR142948TFA在HT-29細(xì)胞中拮抗NT誘導(dǎo)的肌醇單磷酸鹽形成，IC50為3.9nM。SR142948TFA在體內(nèi)阻斷NT誘導(dǎo)的體溫過低、鎮(zhèn)痛和轉(zhuǎn)向?為。SR142948TFA可以透過?腦屏障，可?于精神疾病的研究[1][2]。體外研究SR142948(1μM;90min)TFAinhibitsexpressionofc-fosandkrox24inCHO-hNT1-Rcells[1].SR142948(0-1μM;1h)TFAexhibitsgoodantagonisticactivitybyinhibiting[125I-Tyr3]NTbindstoh-NTR1-CHOandHT29cellmembranes,withIC50sof1.19and0.32nM,respectively[2].SR142948(0-1μM;30min)TFAantagonizesproductionofIP1stimulatedbyNTbothinh-NTR1-CHOandHT29cells,inaconcentration-dependentmanner[2].SR142948(1,10nM;60-80s)TFAantagonizesintracellularcalciummobilizationstimulatedbyNTinh-NTR1-CHOcells[2].體內(nèi)研究SR142948(2μg/kg;p.o.;single)TFAinhibitstheturningbehaviorinducedbyNT(10pg/mouse)[2].SR142948(0.01,0.03,0.3mg/kg;i.p.;single)TFApreventstheenhancementofAChreleaseproducedbyNT(100nM),inadose-dependentmanner[2].SR142948(0-10mg/kg;p.o.;single)TFApartiallybutsignificantlyblocksNT-inducedhypothermia(53%at2mg/kginratsand54%at4mg/kginmice)[2].REFERENCES[1].PortierM,etal.Neurotensintype1receptor-mediatedactivationofkrox24,c-fosandElk-1:preventingeffectoftheneurotensinantagonistsSR48692andSR142948.FEBSLett.1998Jul31;432(1-2):88-93.1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[2].GullyD,etal.BiochemicalandpharmacologicalactivitiesofSR142948A,anewpotentneurotensinreceptorantagonist.JPharmacolExpTher.1997Feb;280(2):802-12.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:4