Geranylgeraniol-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGeranylgeraniolCat.No.:HY-W011474CASNo.:24034-73-9分⼦式:C₂₀H₃₄O分⼦量:290.48作⽤靶点:NF-κB作⽤通路:NF-κB储存⽅式:Pureform-20°C3years4°C2yearsInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY⽣物活性Geranylgeraniol⼀种⼝服有效的维⽣素K2亚型，甲戊酸途径(mevalonatepathway)的中间体。Geranylgeraniol靶向NF-kB信号通路，可在动物模型中减轻脂多糖(LPS)诱导的⼩胶质细胞炎症。IC50&TargetNF-kB[1]体外研究Geranylgeraniol(0-10μM;24h)dose-dependentlysuppressestheLPS-inducedincreaseinthemRNAlevelsofIl-1β,Tnf-α,Il-6,andCox-2[1].Geranylgeraniol(10μM;24h)inhibitsthephosphorylationofTAK1,IKKα/β,andNF-κBp65proteinsaswellasNF-κBnucleartranslocationinducedbyLPSwhilemaintainingIκBαexpression[1].Geranylgeraniol,(50μM;24h)eliminatescelldamagecausedbySimvastatin(HY-17502)(10µM)andMevalonat(10mM),andreducestheinflammatorymarkerandthedamageofthemitochondria,maintainingitsshapeandcomponent[2].WesternBlotAnalysis[1]CellLine:MG6cellConcentration:0,1,10μMIncubationTime:24hoursResult:SuppressedbyTAK1,IKKα/β,andNF-κBp65proteinslevelat10μM.1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemERT-PCR[1]CellLine:MG6cellConcentration:10μMIncubationTime:0,6,12,24hoursResult:Significantlyinhibitedpro-inflammatorycytokineIl-1β,Tnf-α,Il-6,andCox-2mRNAlevel.体内研究Geranylgeraniol(725mg/kg/d;p.o.;90d)isnottoxicologicallysignificantwithadosebelow725mg/kg/dinrats[3].Geranylgeraniol(483mg/kg/d;p.o.;10d)suppresseslipopolysaccharide-inducedinflammationviainhibitionofnuclearfactor-κBactivationinrats[4].AnimalModel:HanWistarrats(169-192gformale;116-152gforfemale)[3]Dosage:0,725,1450,and2900mg/kgAdministration:Oralgavage;oncedaily;90daysResult:Showedthelowestobservedadverseeffectlevel(LOAEL)forlocaleffectsandthenoobservedadverseeffectlevel(NOAEL)forsystemiceffectsas725mg/kg/d.Reducedbodyweightsby12.9and21.6%intheintermediate-andhigh-dosegroupmales,respectively,comparedtocontrols.AnimalModel:Wistarrats(male,8-week-old,130-150g)[4]Dosage:0,48.3,483,4830mg/kgAdministration:Oralgavage;oncedaily;10days;withornotLPSchallenge(i.p.;0.5mg/kg)Result:SuppressedLPS-inducedinflammatorycytokinesandmRNAexpressionofLPS-inducedinflammatorygenesinliverwithdosesof483mg/kgand4830mg/kg.SuppressedproteinlevelsofIRAK1,TRAF6,andTAK1,originatingfromtranscriptionaldown-regulationwithdosesof483mg/kgand4830mg/kg.REFERENCES[1].SaputraWD,etal.GeranylgeraniolInhibitsLipopolysaccharide-InducedInflammationinMouse-DerivedMG6MicroglialCellsviaNF-κBSignalingModulation.IntJMolSci.2021Sep29;22(19):10543.[2].MarcuzziA,etal.GeranylgeraniolandNeurologicalImpairment:InvolvementofApoptosisandMitochondrialMorphology.IntJMolSci.2016Mar11;17(3):365.[3].PreeceK,etal.Atoxicologicalevaluationofgeranylgeraniol.RegulToxicolPharmacol.2021Aug;124:104975.[4].GiriwonoPE,etal.Dietarysupplementationwithgeranylgeraniolsuppresseslipopolysaccharide-inducedinflammationviainhibitionof2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEnuclearfactor-κBactivationinrats.EurJNutr.2013Apr;52(3):1191-9.McePdfHeightCaution:Producthasnotbeenf