Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEvodiamineCat.No.:HY-N0114CASNo.:518-17-2Synonyms:(+)-Evodiamine;d-Evodiamine分?式:C??H??N?O分?量:303.36作?靶點(diǎn):Others作?通路:Others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:10mg/mL(32.96mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.2964mL16.4821mL32.9641mL5mM0.6593mL3.2964mL6.5928mL10mM0.3296mL1.6482mL3.2964mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoil1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥1mg/mL(3.30mM);ClearsolutionBIOLOGICALACTIVITY?物活性Evodiamine從吳茱萸的果實(shí)中分離的?物堿,具有多種?物活性，?如抗炎，抗肥胖和抗腫瘤。體外研究Evodiamineshowscytotoxicityagainstavarietyofhumancancercell-linesbyinducingapoptosis.Moreover,itisanaturallymulti-targetingantitumormolecule,whichexertstheantitumoractivitybyvariousmolecularmechanismsuchascaspase-dependentand-independentpathways,sphingomyelinpathway,calcium/JNKsignaling,31PI3K/Akt/caspaseandFas-L/NF-κBsignalingpathways32[1].體內(nèi)研究Evodiamineinhibitsthemetabolismofdapoxetine.Comparedtothecontrolgroup,thepharmacokineticparameteroft1/2,AUC(0-∞)andTmaxofdapoxetineinevodiaminegroupissignificantlyincreasedby63.3%,44.8%and50.4%,respectively.Moreover,evodiaminehassignificantlydecreasedthepharmacokineticparameteroft1/2andAUC(0-∞)ofdesmethyldapoxetine[2].EvodiaminesuppressestumorgrowthinasubcutaneousH22xenograftmodel.EvodiamineattenuatesVEGF-inducedangiogenesisinvivo[3].PROTOCOLCellAssay[1]EvodiamineisdissolvedinDMSOanddilutedwithappropriatemediumbeforeuse.Theevodiamine-inspirednewscaffoldsareassayedforgrowthinhibitoryactivitiestowardhumancancercell-linesA549(lungcancer),MDA-MB-435(breastcancer)andHCT116(coloncancer)usingtheMTTassay.Evodiamineandcamptithecinareusedasreferencedrugs[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats:TwelvehealthymaleSprague-Dawleyratsarerandomlydividedinto2groups:thecontrolgroupAdministration[2][3](receivedoral10mg/kgdapoxetinealone)andthecombinationgroup(10mg/kgdapoxetineorallyco-administeredwith100mg/kgevodiamine).Theplasmaconcentrationofdapoxetineanddesmethyldapoxetineareestimatedbyultra-performanceliquidchromatography-tandemmassspectrometry(UPLC-MS/MS),anddifferentpharmacokineticparametersarecalculated[2].Mice:Anudemousexenograftmodelisestablishedbyusing4–6-week-oldmaleBALB/cnudemice.Micearedoseddailywith20mg/kg(10mL/kg)ofevodiamineintragastrically,sixmicearedosedintraperitoneallywith10mg/kgof5-flurouracil(5-FU)twiceaweek,andsixmicearenottreated.Thetumorvolumesaredeterminedbymeasuringtwodimensions,withtumorvolume=length×width×width/2.After2or3weeksoftreatment,micearesacrificedbycervicaldislocationunderanesthesiawithether,andthetumortissuesarecollected[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?PharmacolRes.2020May;155:104751.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?Phytomedicine.10October2022,154493.?PhytotherRes.2021Mar3.?JEthnopharmacol.2022Aug2;115586.?OncolLett.2020Oct;20(4):121.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WangS,etal.ScaffoldDiversityInspiredbytheNaturalProductEvodiamine:DiscoveryofHighlyPotentandMultitargetingAntitumorAgents.JMedChem.2015Aug27;58(16):6678-96.[2].LiRF,etal.EffectsofEvodiamineonthePharmacokineticsofDapoxetineandItsMetaboliteDesmethylDapoxetineinRats.Pharmacology.2016;97(1-2):43-7.[3].ShiL,etal.Evodiamineexertsanti-tumoreffectsagainsthepatocellularcarcinomathroughinhibitingβ-catenin-mediatedangiogenesis.TumourBiol.2016Sep;37(9):12791