COH-SR4-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECOH-SR4Cat.No.:HY-124822CASNo.:73439-19-7分?式:C??H?Cl?N?O分?量:350.03作?靶點(diǎn):AMPK作?通路:Epigenetics;PI3K/Akt/mTOR儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(357.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8569mL14.2845mL28.5690mL5mM0.5714mL2.8569mL5.7138mL10mM0.2857mL1.4284mL2.8569mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.08mg/mL(5.94mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.94mM);ClearsolutionBIOLOGICALACTIVITY?物活性COH-SR4?種AMPK活化劑。COH-SR4對??病、??素瘤、乳腺癌和肺癌顯?出強(qiáng)?的抗增殖活性。COH-SR4通過激活A(yù)MPK來抑制脂細(xì)胞分化，有望?于肥胖及代謝紊亂相關(guān)的研究[1]。IC50&TargetAMPK[1]體外研究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.體內(nèi)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?邊的抑制劑?師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