racemic-Equol-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE(±)-EquolCat.No.:HY-100583ACASNo.:94105-90-5分⼦式:C₁₅H₁₄O₃分⼦量:242.27作⽤靶点:EstrogenReceptor/ERR;DrugMetabolite作⽤通路:Others;MetabolicEnzyme/Protease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)*"≥"meanssoluble,butsaturationunknown.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(±)-Equolequol的外消旋体。(±)-Equol对ERα和ERβ的EC50sof分别为200和74nM。Equol⼤⾖异酮⾖苷和⼤⾖素的代谢产物。体外研究Equolisfirstisolatedandidentifiedfrompregnant-mares'urineandlaterfoundintheurineofthegoat,cow,henandsheep[1].Equol,unlikethesoyisoflavonesdaidzeinorgenistein,hasachiralcenterandthereforecanoccuras2distinctdiastereoisomers.S-equolistheexclusiveproductofhumanintestinalbacterialsynthesisfromsoyisoflavonesandbothenantiomersarebioavailable.S-equolhasahighaffinityforestrogenreceptorbeta(Ki=0.73nM),whereasR-equolisrelativelyinactive[2].EquolcouldpromotetheproliferationanddifferentiationofratosteoblaststhroughactivatingtheER-PKCα-relatedsignalingpathway.Thealkalinephosphataseactivityalsoincreasessignificantlyinalloftheequoland17β-estradiol(E2)groups.Equolalsosignificantlyelevatestheosteocalcinlevels[3].体内研究Equolisamodestnatriureticandvasorelaxantagentintherat.Orallyadministeredequolisabout8-foldlesspotentthanorallyadministeredfurosemide.Inisolatedaorticringsprecontractedbyadministrationofphenylephrine,administrationofequolrelaxesthecontractedaorta(concentrationforhalf-maximalactivity58.9±16μM)[4].EquolpossessesanticanceractivitythatsuppressestumorformationviaapoptosisinductioninratswithDMBA-inducedmammaryglandtumors.Inaddition,equolshowsahepaticprotectiveeffectbyactingasanantioxidantandbyreducingapoptosis[5].PROTOCOLCellAssay[3]Primaryratosteoblastsaretreatedwith0.01-1μMequol,0.01-1μME2,or0.01-1μMequol/E2combinedwith1μMICI182780for24or48hours.Then10mL5mg/mLMTTsolutionisaddedtoeachwell.Theplatesareincubatedat37°Cfor4h,andthenthesupernatantisdiscardedand100mLDMSOisaddedtoeachwellandmixedthoroughlybeforetakingmeasurementsinamicroplatereader[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats:Equolorfurosemideisadministeredorallyatdosesof16,40,and100mg/kg(inavolumeof16mL/kgAdministration[3][5]5%arabicsyrup)togroupsof3-9rats(ratsofacontrolgroupareadministeredvehicleonly).Urinesamplesarecollectedfor6h.Urinarysodiumandpotassiumcontentsaremeasuredbyflamephotometry[3].Mouse:Equolisdissolvedinwaterandadministeredorallytoratsatadoseof5and25mg/kgBWfor8weeksafterasingledoseofDMBA(100mg/kg).Ascontrols,ratsaredividedintovehiclealoneandDMBAalonegroups.Inthesecondpart,ICRmiceareorallyadministeredequoldailyatadoseof5and25mg/kgBWfor7weeksbeforeasingledoseofDMBA(34mg/kg/week).Afterequoladministrationanimalsare2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEfollowedfor1weekcontinuously.Thecontrolgroupsarethesameasaboveandeachgrouparecomprisedofsixmice.Miceliversandmammaryglandtumorsareisolated,blotted,weighed,frozeninliquidnitrogenandstoredat-70°Cuntilassayed[5].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].AxelsonM,etal.Theidentificationoftheweakoestrogenequol[7-hydroxy-3-(4'-hydroxyphenyl)chroman]inhumanurine.BiochemJ.1982Feb1;201(2):353-7.[2].SetchellKD,etal.S-equol,apotentligandforestrogenreceptorbeta,istheexclusiveenantiomericformofthesoyisoflavonemetaboliteproducedbyhumanintestinalbacterialflora.AmJClinNutr.2005May;81(5):1072-9.humanintestinalbacterialfl[3].WangJ,etal.Equolpromotesratosteoblastproliferationanddifferentiationthroughactivatingestrogenreceptor.GenetMolRes.2014Jul4;13(3):5055-63.[4].GimenezI,etal.Renalandvascularactionsofequolintherat.JHypertens.1997Nov;15(11):1303-8.[5].ChoiEJ,etal.Anticancermechanismofequolin7,12-dimethylbenz(a)anthracene-treatedanimals.IntJOncol.2011Sep;39(3):747-54.[6].CharoenthongtrakulS,etal.Enhancedgastrointestinalmotilitywithorallyactiveghrelinre