Coronarin-A-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECoronarinACat.No.:HY-N3628CASNo.:119188-33-9分⼦式:C₂₀H₂₈O₂分⼦量:300.44作⽤靶点:mTOR;RibosomalS6Kinase(RSK)作⽤通路:PI3K/Akt/mTOR;MAPK/ERKPathway储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性CoronarinA⼀种具有⼝服活性的天然物，可抑制mTORC1和S6K1增加IRS1活性。CoronarinA具有抗炎活性，也可⽤于糖尿病的研究。IC50&TargetmTORC1S6K1体外研究CoronarinA(3-30ꢀμM;4or12h)stimulatesglycogensynthesisthroughactivatingPI3K/Akt/GSK3βsignalingandinhibitsgluconeogenesisbyactivatingERK-dependentWnt/β-catenin/TCF7L2pathwayinratprimaryhepatocytes[1].CoronarinA(1-30μM;4h)increasestyrosinephosphorylationofIRS1throughinhibitingmTOR/S6K1signaling[1].WesternBlotAnalysis[1]CellLine:PrimaryrathepatocytesConcentration:1,3,10and30μMIncubationTime:4hResult:IncreasedtheAktandGSK3βphosphorylationdose-dependently.Dose-dependentlystimulatedthephosphorylationofbothERK1andERK2.Increasedthephosphorylationofβ-cateninandmitogen-activatedproteinkinasekinase(MEK).Dose-dependentlyenhancedthetyrosinephosphorylationofIRS1atTyr1222,whereastheserinephosphorylationofIRS1wasdose-dependentlyinhibited.Reducedthephosphorylation1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEofmTOR,S6K1andS6.CellViabilityAssay[1]CellLine:PrimaryrathepatocytesConcentration:1,3,10,30,100and300μMIncubationTime:5.5hor12hResult:Showednotoxicityat1-30μM,decreasedcellviabilityafter12hincubationat100μM.体内研究CoronarinA(30or100mg/kg;i.p.orp.o.;oncedailyfor22days)ameliorateshyperglycemiainmice[1].CoronarinA(100mg/kg;p.o.;oncedailyfor22days)inhibitsthemTOR/S6K1pathwaytoactivatePI3K/Akt

andERK/β-cateninsignalinginliversofob/obmice[1].PharmacokineticpropertiesofCoronarinAaftersingleadministrationainob/obmice[1].CoronarinAt1/2(h)tmax(h)Cmax(ng/mL)AUC0-t(ng⋅h/mL)AUC0-∞(ng⋅h/mL)MRT(h)i.p.14.81.0107345711104521.7p.o.3.011.0388169418564.88Dataarepresentedasthemeanofthreemice.aCoronarinAwasintraperitoneallyororallyadministeredat30mg/kgtoob/obmice.AnimalModel:Maleob/obmice[1]Dosage:30mg/kg(IP)or100mg/kg(PO)Administration:Oralorintraperitonealadministration,oncedailyfor22daysResult:Significantlydecreasedthenon-fastingandfastingbloodglucose.Significantlyreducedtheseruminsulinconcentrationat15minafterglucoseloading,reducedtheaveragedailyfoodintakewhilethebodyweightwasunaffected.IncreasedhepaticglycogencontentandtheexpressionlevelsofgluconeogenicgenePck1andG6pcweresignificantlydecreased.AnimalModel:Femaleob/obmice[1]Dosage:30mg/kgAdministration:Intraperitonealororaladministration(PharmacokineticAnalysis)Result:Intraperitonealinjectionexhibitedhigherplasmaexposurethanoralgavageatthesamedoseof30mg/kg,withCmaxvalueof1073and388ng/mL,respectively.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].HuangSL,etal.CoronarinAmodulatedhepaticglycogensynthesisandgluconeogenesisviainhibitingmTORC1/S6K1signalingandamelioratedglucosehomeostasisofdiabeticmice.ActaPharmacolSin.2022Sep9.McePdfHeightCaution:Producthasnotbeenfu