Pirenzepine-LS-519-free-base-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPirenzepineCat.No.:HY-17037ACASNo.:28797-61-7Synonyms:LS519freebase;Pirenzepin;Gastrozepin分⼦式:C₁₉H₂₁N₅O₂分⼦量:351.4作⽤靶点:mAChR作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Pirenzepine(LS519freebase)⼀种选择性的M1mAChR(毒蕈碱⼄酰胆碱受体)拮抗剂。Pirenzepine可减少胃酸分泌并减少肌⾁痉挛，可⽤于消化性溃疡的研究。Pirenzepine具有对癌细胞的抗增殖活性。体外研究Pirenzepine(100-140μg/mL;24h)inhibitsPC-3cellproliferationactivity[2].Pirenzepine(110μg/mL;24h)inhibitsprostateandlungcancercellmigration[2].Pirenzepine(100-130μg/mL;0-24h)inhibitstheexpressionofGLI1inPC-3cells[2].CellProliferationAssay[2]CellLine:PC-3cellsConcentration:100-140μg/mLIncubationTime:24hoursResult:InhibitedPC-3cellproliferationinaconcentration-dependentmanner.CellMigrationAssay[2]CellLine:PC-3andA549cellsConcentration:110μg/mLIncubationTime:24hours1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:InhibitedthemigrationofPC-3andA549celllines(P=0.014).WesternBlotAnalysis[2]CellLine:PC-3cellsConcentration:110μg/mLIncubationTime:0-24hoursResult:InhibitedtheexpressionofGLI1andPTCH1.RT-PCR[2]CellLine:PC-3cellConcentration:100-130μg/mLIncubationTime:24hoursResult:SuppressedGLI1mRNAexpressioninPC-3cells.IncreasedPTCH1mRNAlevelbutnotreachstatisticalsignificance.ShowednoSHHmRNAexpressionlevelchange.体内研究Pirenzepine(intraperitonealinjection;0.3ꢀmg/kg;once)treatmentshowsbeneficialeffectsinlipopolysaccharide-inducedsepticshock[3].AnimalModel:MaleC57BL/6micewithexperimentalendotoxemia[3]Dosage:0.3ꢀmg/kgAdministration:Intraperitonealinjection;0.3ꢀmg/kg;onceResult:ImprovedsurvivalrateofLPS-inducedsepticshock.RelievedLPS-inducedpulmonaryandhepaticinjury.ReducedtheexpressionofSOCS3atmRNAlevel.户使⽤本产品发表的科研⽂献•ResearchSquarePreprint.2021Jan.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].CarmineAA,etal.Pirenzepine.Areviewofitspharmacodynamicandpharmacokineticpropertiesandtherapeuticefficacyinpepticulcerdiseaseandotherallieddiseases.Drugs.1985Aug;30(2):85-126.[2].YinQQ,etal.MuscarinicacetylcholinereceptorM1mediatesprostatecancercellmigrationandinvasionthroughhedgehogsignaling.AsianJAndrol.2018Nov-Dec;20(6):608-614.[3].YabukiY,etal.TheT-typecalciumchannelenhancerSAK3inhibitsneuronaldeathfollowingtransientbrainischemiavianicotinicacetylcholinereceptorstimulation.NeurochemInt.2017Sep;108:272-281.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap