COH-SR4-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECOH-SR4Cat.No.:HY-124822CASNo.:73439-19-7分⼦式:C₁₃H₈Cl₄N₂O分⼦量:350.03作⽤靶点:AMPK作⽤通路:Epigenetics;PI3K/Akt/mTOR储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(357.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8569mL14.2845mL28.5690mL5mM0.5714mL2.8569mL5.7138mL10mM0.2857mL1.4284mL2.8569mL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%salineSolubility:2.08mg/mL(5.94mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.94mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性COH-SR4⼀种AMPK活化剂。COH-SR4对⽩⾎病、⿊⾊素瘤、乳腺癌和肺癌显⽰出强⼤的抗增殖活性。COH-SR4通过激活AMPK来抑制脂细胞分化，有望⽤于肥胖及代谢紊乱相关的研究[1]。IC50&TargetAMPK[1]体外研究COH-SR4(1-5μM;24hours)resultsinadose-dependentincreaseinthephosphorylationofAMPKanditssubstrateACCin3T3-L1preadipocytes,aswellasincancercellssuchasHL-60,HeLa,MCF-7[1].COH-SR4(3-5µM;7days)significantlyinhibits3T3-L1adipocytedifferentiationinadose-dependentmanner[1].COH-SR4(1-5μM;24hours)promotescellG1cyclearrest[1].COH-SR4significantlyreducesintracellularlipidaccumulationanddownregulatestheexpressionofkeyadipogenesis-relatedtranscriptionfactorsandlipogenicproteins[1].WesternBlotAnalysis[1]CellLine:3T3-L1preadipocytes,HL-60cells,HeLacells,MCF-7cellsConcentration:1μM,3μM,5μMIncubationTime:24hoursResult:IndirectlyactivatedAMPK.CellCycleAnalysis[1]CellLine:3T3-L1cellsConcentration:1μM,3μM,5μMIncubationTime:24hoursResult:ModulatedthelevelofproteinsactiveduringSandG2phasesofthecellcycle.体内研究COH-SR4(5mg/kg;i.g.;3x/week;for6weeks)reducesbodyweightandfatmassinhighfatdiet(HFD)obesemicewithoutaffectingfoodintake[2].COH-SR4improvesglycemiccontrolanddyslipidemiainHFDobesemice[2].COH-SR4decreasesadiposetissuehypertrophyandaffectscirculatingadipokinelevelsinHFDobesemice[2].COH-SR4preventshepaticlipidaccumulationandfattyliverinHFDobesemice[2].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:Nine-weekoldmaleC57BL/6Jmice[2]Dosage:5mg/kgAdministration:Oralgavage,threetimesaweek,for6weeksResult:DecreasedbodyweightandfatmassinHFDobesemice.REFERENCES[1].JamesLFigarola,etal.Small‑moleculeCOH-SR4inhibitsadipocytedifferentiationviaAMPKactivation.IntJMolMed.2013May;31(5):1166-76.[2].JamesLesterFigarola,etal.COH-SR4ReducesBodyWeight,ImprovesGlycemicControlandPreventsHepaticSteatosisinHighFatDiet-InducedObeseMice.PLoSOne.2013;8(12):e83801.McePdfHeightCaution:Producthasnotbeenfullyvalid