Norisoboldine-hydrochloride-plus-Laurelliptine-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENorisoboldinehydrochlorideCat.No.:HY-N0586ACASNo.:5083-84-1Synonyms:(+)-Laurelliptinehydrochloride分?式:C??H??ClNO?分?量:349.81作?靶點(diǎn):AdenosineReceptor作?通路:GPCR/GProtein儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Norisoboldinehydrochloride?種具有?服活性的天然芳烴受體(AhR)激動(dòng)劑。Norisoboldine作為林參中主的異喹啉類?物堿，可?于類風(fēng)濕性關(guān)節(jié)炎和潰瘍性結(jié)腸炎的研究[1][2]。IC50&TargetAhR[2]體外研究Norisoboldinehydrochloride(1~30μM;0~24hours;CD4+Tcells)activatesAhRunderhypoxicmicroenvironmentandsignificantlydownregulatesmRNAexpressionofmiR-31[2].Norisoboldinehydrochloride(30μM;0~24hours;CD4+Tcells)inhibitsglycolysisinhypoxia[2].Norisoboldinehydrochloride(1~30μM;0~72hours;Tregcells)promotesTregdifferentiationinhypoxia[2].Norisoboldinehydrochloride(10,30μM)facilitatesthedisassociationofHSP90/AhRcomplexes,thenucleartranslocationofAhR,andtheformationofAhR/ARNTcomplexes.NorisoboldinehydrochlorideinducesgenerationofTregcellsinhypoxia[2].WesternBlotAnalysis[2]CellLine:CD4+TcellsConcentration:1~30μMIncubationTime:24hoursResult:ActivatedAhRincellsunderhypoxicmicroenvironment.RT-PCR[2]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:CD4+TcellsConcentration:1~30μMIncubationTime:24hoursResult:SignificantlydownregulatedmRNAexpressionofmiR-31.Immunofluorescence[2]CellLine:CD4+TcellsConcentration:30μMIncubationTime:24hoursResult:Inhibitedglycolysisinhypoxia.Immunofluorescence[2]CellLine:TregcellsConcentration:1~30μMIncubationTime:72hoursResult:PromotedTregdifferentiationinhypoxia.體內(nèi)研究Norisoboldinehydrochloride(10~40mg/kg;p.o.;20days)significantlyreducestheseverityofjointswellinganderythemaduringthecourseoftheexperiment[1].Norisoboldinehydrochloride(40mg/kg;i.g.;10days)inducesenhancementofCYP1A1expressionandsuppressesexpressionsofGlut1andHK2incolons[2].AnimalModel:MaleICRmice(18–22g)Dosage:10~40mg/kgAdministration:P.o.Result:Significantlyreducedtheseverityofjointswellinganderythemaduringthecourseoftheexperiment.AnimalModel:FemaleC57BL/6mice(18–22g)Dosage:40mg/kgAdministration:I.g.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:InducedenhancementofCYP1A1expressionandsuppressedexpressionsofGlut1andHK2incolons.REFERENCES[1].LuoY,etal.Therapeuticeffectofnorisoboldine,analkaloidisolatedfromRadixLinderae,oncollagen-inducedarthritisinmice.Phytomedicine.2010;17(10):726-731.[2].LvQ,etal.Norisoboldine,anaturalAhRagonist,promotesTregdifferentiationandattenuatescolitisviatargetingglycolysisandsubsequentNAD+/SIRT1/SUV39H1/H3K9me3signalingpathway.CellDeathDis.2018;9(3):258.Published2018Feb15.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed