Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDiosminCat.No.:HY-N0178CASNo.:520-27-4分?式:C??H??O??分?量:608.54作?靶點(diǎn):ArylHydrocarbonReceptor作?通路:Immunology/Inflammation儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(164.33mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.6433mL8.2164mL16.4328mL5mM0.3287mL1.6433mL3.2866mL10mM0.1643mL0.8216mL1.6433mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.11mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:2.5mg/mL(4.11mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Diosmin在各種柑橘類?果中發(fā)現(xiàn)的類酮，也芳烴受體(AhR)的激動(dòng)劑。IC50&TargetAhR[1]體外研究TreatmentwithDiosmincausesadosedependentincreaseintheamountofadductsformed(uptoa7-foldincreaseinadductsat5μMDiosmin).At5μM,Diosminincreasesthecytotoxicityof7,12-dimethylbenz(a)anthracene(DMBA),shiftingtheIC50ofDMBAfromanestimated1.2μMto400nM.Diosminisnotcytotoxicinitselfattheconcentrationstested.DiosmincausesanincreaseinCYPIAIactivityinMCF-7cellsinatime-anddose-dependentfashion.Diosmincausesadose-dependentincreaseinCYPIAImRNAafter24hofincubation,causesalong-lastingincreaseinCYPIAImRNAaccumulationthatreachesitspeakafter48hofincubation[1].體內(nèi)研究Diosminsignificantlydecreasesthemalondialdehyde(MDA)levelsandincreasestheactivitiesoftotal-superoxidedismutase(T-SOD),glutathioneperoxidase(GSH-Px),andcatalase(CAT)intheretinaofratscomparewiththeischemiagroup(P[2].PROTOCOLCellAssay[1]MCF-7cellsareplatedat25,000cells/wellin24-wellplates.After24h,themediumischangedtomediumcontaining5μMDiosmin.Afteranadditional24h,themediumisagainchangedwithmediumcontaining5μMDiosmin.After3days,thetotalcellgrowthisassessedbysulforhodamine[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalHealthymaleWistarrats(n=112)weighing180to200?geachareusedinthisstudy.TheanimalsareAdministration[2]randomlyassignedtothefollowing4groups,whichincludecombinationsoftheischemia/reperfusion(I/R)injurymodelorshaminjurywiththei.g.administrationofDiosminorvehiclesolution:sham+vehicle(SV)group,sham+Diosmin(SD)group,model+vehicle(MV)group,andmodel+Diosmin(MD)group.Forintragastricadministration,5?mLof2%Diosminperkilogramweightoftherat,orthesamevolumeofvehiclesolution,isadministeredintragastrically30?minbeforetheonsetofischemia,andthendailyafterI/Rinjuryuntiltheanimalsaresacrificed.Usinganoverdoseofanesthesia,8ratsfromeachgrouparesacrificed24?hafterI/Rinjury,andtheireyeballsharvestedfordeterminationofthemalondialdehyde(MDA)levelandtheactivitiesoftotal-superoxidedismutase(T-SOD),glutathioneperoxidase(GSH-Px),andcatalase(CAT).At7dayspost-I/Rinjury,electroretinograms(ERGs)arerecordedin6ratspergroup.Meanwhile,6ratsineachgrouparerandomlychosenforretrogradelabelingofretinalganglioncells(RGCs),andtheremaining8ratsfromeachgrouparehistopathologicallyexamined[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ActaPharmSinB.2021Jan;11(1):143-155.?Theranostics.2021;11(18):8797-8812.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CiolinoHP,etal.DiosminanddiosmetinareagonistsofthearylhydrocarbonreceptorthatdifferentiallyaffectcytochromeP4501A1activity.CancerRes.1998Jul1;58(13):2754-60.[2].TongN,etal.Diosminprotectsratretinafromischemia/reperfusioninjury.JOculPharmacolTher.2012Oct;28(5):4