R-Equol-plus-Equol-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE(R)-EquolCat.No.:HY-108414CASNo.:221054-79-1Synonyms:(+)-Equol分⼦式:C₁₅H₁₄O₃分⼦量:242.27作⽤靶点:EstrogenReceptor/ERR作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(412.76mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.1276mL20.6381mL41.2763mL5mM0.8255mL4.1276mL8.2553mL10mM0.4128mL2.0638mL4.1276mL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:≥2.5mg/mL(10.32mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(10.32mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(10.32mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性(R)-EquolERα和ERβ的激动剂，Ki值分别为27.4和15.4nM。IC50&TargetKi:27.4nM(ERα),15.4nM(ERβ)[1]体外研究(R)-EquolisanagonistofbothERαandERβwithKisof27.4and15.4nM,respectively[1].(R)-Equolinducesadose-dependentinhibitoryeffectontheinvasivecapacityofMDA-MB-231cellsthatissignificantatthehighestconcentrationtested(50μM).Following48-hexposureto(R)-Equol,invasionisreducedby62%(p=0.009,versusuntreatedcells)with50μM(R)-Equol.Matrixmetalloproteinase-2(MMP-2)expressionissignificantlydown-regulatedfollowingtreatmentwith50μM(R)-Equol(p=0.035)[2].体内研究Animalsfed(R)-EquolhaveasignificantlyreducednumberofpalpabletumorsovertimewhencomparewithControls(P=0.002).Furthermore,thenumberofpalpabletumorsformedperratinthe(R)-Equol-fedgroupissignificantlylowerthanthatofratstreatedwithS-(-)equol(P=0.008).(R)-Equol-fedanimalshave43%fewertumorsthanthecontrolgroupandthisdifferenceishighlystatisticallysignificant(P=0.004).Thenumberoftumors/tumor-bearinganimalissignificantlylowerintheanimalsfed(R)-EquolcomparewithControls(3.3±0.4versus5.5±0.5,P=0.004).Atnecropsy,themean(±SEM)tumorweightperanimalfor(R)-Equolfedrats(5.3±1.1mg)issignificantlyreduced(P=0.04)whencomparewithControls(9.9±1.4mg).Feedingthe(R)-Equoldietresultsinsignificantlyincreasedtumorlatency(P=0.003)[3].PROTOCOLCellAssay[2]Cellviabilityisdeterminedusingthewell-establishedMTTassay.Cellsareseeded(1.25×105cells/mL)in96-wellplatesinexperimentalmedium(100μL/well)andincubatedfor48hat37°Cina95%air/5%CO2humidifiedatmosphere.Mediumisthenreplacedwithfreshmediumcontaining(R)-Equol(R-equol)(2.5,10or50μM)orDMSOonlyasacontrol.Following48-hincubation,cellviabilityisassessed[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalToinvestigatethechemopreventiveeffectsofdietary(R)-EquolagainstchemicallyinducedmammaryAdministration[3]cancer,femaleSprague-Dawleyratsbredin-housearefedasoy-freeAIN-93Gdietfrombirthto35daysofage,thenseparatedintodifferentgroups.Group1(Controlgroup,n=40)continuesonthisdiet,whereastheothergroupofanimalsarefedtheAIN-93Gdietsupplementedwith250mg/kgof(R)-Equol(Group3,n=41)beginningonday35untilkillingonday190[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].SetchellKD,etal.S-equol,apotentligandforestrogenreceptorbeta,istheexclusiveenantiomericformofthesoyisoflavonemetaboliteproducedbyhumanintestinalbacterialflora.AmJClinNutr.2005May;81(5):1072-9.[2].MageePJ,etal.Daidzein,R-(+)equolandS-(-)equolinhibittheinvasionofMDA-MB-231breastcancercellspotentiallyviathedown-regulationofmatrixmetalloproteinase-2.EurJNutr.2014Feb;53(1):345-50.[3].BrownNM,etal.Thechemopreventiveactionofequolenantiomersinachemicallyinducedanimalmodelofbreastcancer.Carcinogenesis.2010May;31