Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPalvanilCat.No.:HY-137988CASNo.:69693-13-6分?式:C??H??NO?分?量:391.59作?靶點:Others作?通路:Others儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Palvanil?種Capsaicin(HY-10448)類似物，對TRPV1受體表現(xiàn)出較強的脫敏能?，其具有抗疼痛和抗炎作?。體外研究Palvanil(0.1-1000nM;0-300min)leadstocalciumincreasmentinHEK-293intracellular[1].Palvanil(1-10nM;5min)treatmentdesensitizesTRPV1totheeffectofCapsaicinsignificantly[1].CellViabilityAssay[1]CellLine:HEK-293cellsConcentration:0.1,0.5,1,5,10,50,100and1000nMIncubationTime:0-300minResult:Producedadose-dependentincreaseinintracellularcalciumwithaEC50of0.65nM.CellViabilityAssay[1]CellLine:HEK-293-TPRV1cellsConcentration:1-10nMIncubationTime:5minResult:DesensitizedTRPV1totheeffectofCapsaicinsignificantly(IC50=0.81nM).1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體內(nèi)研究Palvanil(subcutaneousinjection;1or10mg/kg;once)treatmentshowshypothermiceffect[2].Palvanil(intraperitonealinjection;100μL(15nM)permouse;once)treatmentreducesCapsaicin-inducedbronchoconstriction[2].Palvanil(intravenousinjection;0.5,0.75,and1mg/kg;once)treatmentshowsantinociceptiveeffectsonFormalin-inducednocifensivebehavior[2].Palvanil(intravenousinjection;0.5,0.75,and1mg/kg;once)treatmentinhibitsCarrageenan-inducedinflammation[2].Palvanil(intravenousinjection;0.5and1mg/kg;oncedaily;7days)reducesmechanicalallodyniaandthermalhyperalgesiainsparednerveinjury(SNI)mice[2].AnimalModel:MaleCD-1mice[2]Dosage:1or10mg/kgAdministration:Subcutaneousinjection;1or10mg/kg;onceResult:Ledtoaslightandshortlastinghypothermiceffect,producedlatehyperthermia.AnimalModel:FemaleBALB/Cmice[2]Dosage:100μL(15nM)permouseAdministration:Intraperitonealinjection;100μL(15nM)permouse;onceResult:Inducedasignificantlylowerbronchoconstriction(from0.47to0.605cmH2O/L/s).AnimalModel:MaleCD-1micereceivedformalin[2]Dosage:0.5,0.75,and1mg/kgAdministration:Intravenousinjection;0.5,0.75,and1mg/kg;onceResult:ReducedthesecondphaseofFormalin-inducednociceptivebehaviourinadose-dependentmanner.AnimalModel:MaleC57BL/6JmicewithacuteinflammationinducedbyCarrageenan[2]Dosage:2.5mg/kgAdministration:Intravenousinjection;2.5mg/kg;onceResult:Reducedthevolumeoftheoedemaintheipsilateralhindpaw(64%).AnimalModel:MaleCD-1mice[2]Dosage:0.5and1mg/kg2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAdministration:Intravenousinjection;0.5and1mg/kg;oncedaily;7daysResult:Reducedmechanicalallodyniaandthermalhyperalgesiaat3and7daysafternerveinjuryinadose-dependentmanner.REFERENCES[1].LucianoDePetrocellis,etal.N-palmitoyl-vanillamide(palvanil)isanon-pungentanalogueofcapsaicinwithstrongerdesensitizingcapabilityagainsttheTRPV1receptorandanti-hyperalgesicactivity.PharmacolRes.2011Apr;63(4):294-9.[2].LivioLuongo,etal.Palvanil,anon-pungentcapsaicinanalogue,inhibitsinflammatoryandneuropathicpainwithlittleeffectsonbronchopulmonaryfunctionandbodytemperature.PharmacolRes.2012Sep;66(3):243-50.McePdfHeightCaution:Producthasnotbeenf