Nobiletin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENobiletinCat.No.:HY-N0155CASNo.:478-01-3分⼦式:C₂₁H₂₂O₈分⼦量:402.39作⽤靶点:ROR;ReactiveOxygenSpecies;Apoptosis;Autophagy作⽤通路:MetabolicEnzyme/Protease;Immunology/Inflammation;NF-κB;Apoptosis;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(124.26mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4852mL12.4258mL24.8515mL5mM0.4970mL2.4852mL4.9703mL10mM0.2485mL1.2426mL2.4852mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(5.17mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.21mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.17mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Nobiletin⼀种来⾃柑橘⽪的聚甲氧酮，可改记忆⼒丧失，⼀种RORs激动剂。Nobiletin可以降低分化的C2C12肌管中的ROS的⽔平，并具有抗炎和抗癌特性，包括抗⾎管⽣成，抗增殖，抗转移和诱导细胞凋亡。IC50&TargetRetinoidacidreceptor-relatedorphanreceptors(RORs)[1];reactiveoxygenspecies(ROS)[1];apoptosis[2]体外研究Nobiletin(0-100μM;24hours;U2OSandHOScells)treatmentprogressivelyreducesproteinexpressionsofMMP-2andMMP-9.InU2OSandHOScells,Nobiletinconsiderablyreducesthephosphorylationofp-IKKα/βandp-IκBα,andproteinexpressionofNF-κBinthecellnuclearfractionwiththeconcomitantincreaseoftheNF-κBexpressioninthecytosolicfraction.Nobiletindown-regulatesthep-CREBandtheSP-1expressionsinthenuclearfraction,whereasNobiletindoesnotaffectc-Junandc-Fosexpressions[1].Nobiletin(0-100μM;24hours;U2OSandHOScells)treatmentsignificantlyreducesmRNAexpressionsofMMP-2andMMP-9dose-dependentlyinU2OSandHOScells[1].WesternBlotAnalysis[1]CellLine:U2OSandHOScellsConcentration:0μM,25μM,50μM,75μM,100μMIncubationTime:24hoursResult:ProgressivelyreducedproteinexpressionsofMMP-2andMMP-9.Considerablyreducedthephosphorylationofp-IKKα/βandp-IκBα,andproteinexpressionofNF-κBinthecellnuclearfractionwiththeconcomitantincreaseoftheNF-κBexpressioninthecytosolicfraction.Down-regulatedthep-CREBandtheSP-1expressionsinthenuclearfractioninU2OSandHOScells.RT-PCR[1]CellLine:U2OSandHOScellsConcentration:0μM,25μM,50μM,75μM,100μMIncubationTime:24hoursResult:SignificantlyreducedmRNAexpressionsofMMP-2andMMP-9dose-dependentlyinU2OSandHOScells.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究Nobiletin(0.1%ofregulardiet;oraladministration;daily;for20weeks;maleC57BL/6mice)treatmentrestoresglucosehomeostasisandpromotsenergyexpenditureandcircadianactivityinagedmice[2].AnimalModel:20-to22-month-oldmaleC57BL/6mice[2]Dosage:0.1%ofregulardietAdministration:Oraladministration;daily;for20weeksResult:Fullyrestoredglucosetoleranceinagedmice,andincreasedbasalbodytemperatureandcoldtoleranceinagedmice.Ledtoatwofoldincreaseindistancerun/dayonvoluntarywheelscomparedwithagedregulardiet-fedmiceduringtheactivephase.户使⽤本产品发表的科研⽂献•ActaPharmSinB.2021Jan;11(1):143-155.•IntJBiolSci.2022Sep11;18(15):5698-5712.•JAgricFoodChem.2022Feb9;70(5):1536-1546.•SciRep.2021Jun3;11(1):11796.•BiolReprod.2021Oct7;ioab184.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ChengHL,etal.NobiletininhibitshumanosteosarcomacellsmetastasisbyblockingERKandJNK-mediatedMMPsexpression.Oncotarget.2016Jun7;7(23):35208-23.[2].NoharaK,etal.Nobiletinfortifiesmitochondrialrespirationinskeletalmuscletopromotehealthyagingagainstmetabolicchallenge.NatCommun.2019Aug28;10(1):3923.[3].HeB,etal.TheSmallMoleculeNobiletinTargetstheMolecularOscillatortoEnhanceCircadianRhythmsandProtectagainstMetabolicSyndrome.CellMetab.2016Apr12;23(4):610-21.[4].TakitoJ,etal.NervegrowthfactorenhancestheCRE-dependenttranscriptionalactivityactivatedbynobiletininPC12cells.CanJPhysiolPharmacol.2016