BC1618-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBC1618Cat.No.:HY-134656CASNo.:2222094-18-8分⼦式:C₂₄H₂₄F₃NO₂分⼦量:415.45作⽤靶点:AMPK;Mitophagy;E1/E2/E3Enzyme作⽤通路:Epigenetics;PI3K/Akt/mTOR;Autophagy;MetabolicEnzyme/Protease储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(240.70mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4070mL12.0351mL24.0703mL5mM0.4814mL2.4070mL4.8141mL10mM0.2407mL1.2035mL2.4070mL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>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.5mg/mL(6.02mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.02mM);Clearsolution3.请依序添加每种溶剂：50%PEG300>>50%salineSolubility:5mg/mL(12.04mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性BC1618，具有⼝服活性的Fbxo48抑制剂，可刺激Ampk信号(阻⽌激活的pAmpkα被Fbxo48介导的蛋⽩酶体降解)。BC1618促进线粒体分裂、促进⾃噬，提⾼肝脏胰岛素的敏感性。体外研究BC1618enhancespAmpkαproteinstabilityduringCHXtreatment[1].BC1618displaysmorethan1,000-foldenhancedactivitytostimulatepAmpkαincellsthanmetformin[1].BC1618(0.1-2μM,16h)induceddose-andtime-dependentincreasesinpAmpkαandpACCproteinlevelsarealsoconfirmedinhumanprimary-likehepatocytes[1].BC1618(1μM)effectivelydisruptstheinteractionbetweenFbxo48andpAmpkα,andhasnoeffectonFbxo48,Ampkα1orAmpkα2messengerRNAs[1].BC1618increasestheabundanceofaseriesofautophagicmarkerproteinsduringglucosedepletion.BC1618inducesphosphorylationofthemTORC1associatedproteinRaptor,reducingpS6levels,allconsistentwiththeknownmTORinhibitoryeffectsexertedbyactivatedAmpk[1].WesternBlotAnalysis[1]CellLine:BEAS-2Bcells.Concentration:0-2μM.IncubationTime:16h.Result:InducedpAmpkαandpACCproteinlevelsdose-dependently.体内研究BC1618promotesmitochondrialfission,facilitatesautophagyandimproveshepaticinsulinsensitivityinhigh-fat-diet-inducedobesemice[1].BC1618,appearstobe~1,000-foldmorepotentthanmetforminandisextremelywelltoleratedinmice[1].BC1618displaysexcellentoralbioavailabilitywithapeakof2,000ng/mLwithin0.5hand500ng/mLinplasmaat4hafteranoralloadof20mg/kg[1].AnimalModel:C57BL/6mice[1].Dosage:2or10mg/kg(challengedwithLPS(3mg/kg)foranadditional18h).Administration:IP,once.Result:Reducedlunginflammationinendotoxintreatedmice.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:C57BL/6mice[1].Dosage:15and30mg/kg/d.Administration:Drinkingwaterfor3months.Result:Exhibitednoobvioustoxicity.REFERENCES[1].YuanLiu,etal.AFbxo48inhibitorpreventspAMPKαdegradationandamelioratesinsulinresistance.NatChemBiol.2021Mar;17(3):298-306.McePdfHeightCaution:Producthasnotbeenfullyv