TJN-331-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETJN-331Cat.No.:HY-178850CASNo.:219964-53-1分⼦式:C₁₉H₂₂N₂O₃分⼦量:326.39作⽤靶点:TGF-βReceptor作⽤通路:TGF-beta/Smad储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性TJN-331⼀种强效且⼝服有效的TGF-β1抑制剂。TJN-331通过抑制TGF-β1的产⽣，改⼤⿏抗肾⼩球基底膜(GBM)肾炎，从⽽减少肾⼩球⽑细⾎管外增⽣。TJN-331可抑制ddY⼩⿏实验性IgA肾病模型中的系膜扩张。TJN-331可⽤于肾炎和IgA肾病的研究[1][2]。体外研究TJN-331(1-50μmol/L;24-48h)dose-dependentlyinhibitstotalandmatureTGF-β1productionandreversesthedecreaseinSmad2andSmad3mRNAexpression,andinhibitsplasminogenmRNAexpressioninisolatedglomerulifromanti-GBMnephriticrats[1].TJN-331(10-100μmol/L;48hours)dose-dependentlyinhibitsTGF-β1productionfromsplenocytesstimulatedwithConA[2].体内研究TJN-331(0.1,0.5,and2.0mg/kg;p.o.;oncedailyfor21daysfromday21today41)reducesproteinuriaandhistopathologicalchanges,andinhibitsTGF-β1proteinproductionandpositiveareasintheanti-GBMinducednephriticratmodel[1].TJN-331(0.1,0.5,and2.0mg/kg;p.o.;dailyfor5weeksfromweek10toweek15)improvesrenalfunctionandhistopathologicalchangesinglomeruliinanIgAnephropathymodelinmice[2].AnimalModel:MaleSDratsinjectedwithgoatγ-globulinandgoatanti-ratGBMserum[1]Dosage:0.1,0.5,and2.0mg/kgAdministration:p.o.;dailyfor21daysfromday21today41Result:Preventedurinaryproteinexcretionat2mg/kgfromday30today41,andshowed1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEsignificantinhibitiononlyatday35at0.5mg/kg.showedatendencytoinhibitnephritisinducedincreaseinserumcreatininelevels.Inhibitedcrescentformationandadhesionintheanti-GBMnephriticglomeruliat2mg/kg.Inhibitedtheincreaseofa-SmoothMuscleActin(SMA)andTGF-β1-positiveareas.Inhibitedtheincreaseinglomerularproductionofmatureat2mg/kg.AnimalModel:MaleddYmice(7-week-old)inducedbyoraladministrationofbovineγ-globulin,followedbyreticuloendothelialblockingbycolloidalcarboninjectionandheminephrectomy.[2]Dosage:0.1,0.5,and2.0mg/kgAdministration:p.o.;dailyfor5weeks(fromweek10toweek15afterinduction)Result:Inhibitedincreasesinthemesangialmatrixindexandthenumberofnucleiperglomerularcross-section.PreventedincreaseinglomerularTGF-β1stainingwithoutaffectingIgAdeposition.Didnotinfluenceurinevolumeduringtheexperiments.REFERENCES[1].SaegusaY,etal.TJN-331improvesanti-glomerularbasementmembranenephritisbyinhibitingtheproductionofintraglomerulartransforminggrowthfactor-beta1.BiolPharmBull.2010;33(8):1349-1354.[2].SaegusaY,etal.(E)-N-[(3,4-dimethoxyphenethyl)]-N-methyl-3-(3-pyridyl)-2-propenamide(TJN-331)inhibitsmesangialexpansioninexperimentalIgAnephropathyinddYmice.ClinExpNephrol.2010Dec;14(6):528-35.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform