Baicalein-5-6-7-Trihydroxyflavone-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBaicaleinCat.No.:HY-N0196CASNo.:491-67-8Synonyms:5,6,7-Trihydroxyflavone分?式:C??H??O?分?量:270.24作?靶點(diǎn):XanthineOxidase;InfluenzaVirus;Ferroptosis作?通路:MetabolicEnzyme/Protease;Anti-infection;Apoptosis儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(185.02mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.7004mL18.5021mL37.0041mL5mM0.7401mL3.7004mL7.4008mL10mM0.3700mL1.8502mL3.7004mL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(protectfromlight)。-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：0.5%CMC-Na/salinewaterSolubility:20mg/mL(74.01mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.5mg/mL(9.25mM);Clearsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(9.25mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Baicalein(5,6,7-Trihydroxyflavone)IC50值為3.12μM。IC50&TargetIC50:3.12μM(xanthineoxidase)[1]體外研究BaicaleinsuppressesmitogeninducedTcellproliferationandcytokinesecretioninvitro.Pre-treatmentwithbaicaleinsignificantlysuppressesConAoranti-CD3/CD28mAbinducedproliferationaswellascytokinesecretionat25μM.BaicaleintreatmentinducesDNAbindingofNF-κBbutinhibitsthioredoxinactivityinthenuclearcompartment[2].Baicaleinsuppressesproliferation,migration,andinvasionofMDA-MB-231cellsinatime-anddose-dependentmanner.BaicaleinsignificantlydecreasestheexpressionofSATB1inMDA-MB-231cells.BaicaleinalsodownregulatestheexpressionofWnt1andβ-cateninproteinsandtranscriptionlevelofWnt/β-catenin-targetedgenes[3].體內(nèi)研究BaicaleinsuppressesinductionofgraftversushostdiseasebutdoesnotinhibithomeostaticproliferationofT-cellsinmice.Thisobservationclearlyshowspotentanti-inflammatoryactivityofbaicaleininvivo[2].Ratstreatedwithbaicaleinareprotectedagainstanincreaseinhearttobodyweightratio,plasmalevelofbrainnatriureticpeptides,intraventricularseptumthickness,myocardialcollagenvolumeofleftventricle(allP[4].PROTOCOLCellAssay[3]MTTassayisconductedtoevaluatetheeffectofbaicaleinonproliferationofbreastcancercells.MDA-MB-231cellsareroutinelydigested,collected,andthenseededin96-wellplatesatadensityof8×103cells/well.Afterincubationfor12-24hours,cellsaretreatedwith0,20,40,60,80,100,and120μMbaicaleinaccordingtotheirexperimentalgroupingandthenincubatedat37°Cfor24,48,and72hours[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats:Baicaleinissuspendedin1%methylcellulose.RatsaretreatedwithbaicaleinsuspensionviaoralAdministration[2][4]garvage.SHRandWKYratsaredividedinto4groups(n=8pergroup):12-weektreatmentwithhigh-dose(200mg/kg/day)orlow-dose(50mg/kg/day)group;and4-weektreatmentwithhigh-doseorlow-dosegroup.The12-weekand4-weeknegativecontrolgroupsofSHRandWKYrats(n=8pergroup)receivevehiclewhilepositivecontrolgroups(Valgroup,n=8pergroup)receivevalsartan(20mg/kg/day)forcomparison[4].Mice:Tostudytheinvivoanti-inflammatoryefficacyofbaicalein,graft-versus-hostdisease(GVHD)modelisused.SpleniclymphocytesfromC57BL/6miceareincubatedwithbaicaleininvitro(25μM,4h)andadoptivelytransferredtoimmune-compromisedBalb/cmice[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)?Theranostics.2021Jul13;11(17):8301-8321.?OxidMedCellLongev.2022Feb9;2022:4295208.?ActaPharmacolSin.2021Oct20.?Aging(AlbanyNY).2021Jul1;13(13):17370-17379.?JInflammRes.2021Dec16;14:6939-6958.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ShiehDE,etal.Antioxidantandfreeradicalscavengingeffectsofbaicalein,baicalinandwogonin.AnticancerRes.2000Sep-Oct;20(5A):2861-5.[2].PatwardhanRS,etal.Baicaleinexhibitsanti-inflammatoryeffectsviainhibitionofNF-κBtransactivation.BiochemPharmacol.2016May15;108:75-89.[3].MaX,etal.BaicaleinsuppressesmetastasisofbreastcancercellsbyinhibitingEMTviadownregulationofSATB1andWnt/β-cateninpathway.DrugDesDevelTher.2016Apr18;10:1419-41.[4].KongEK,etal.Anovelanti-fibroticagent,baicalein,forthetreatmentofmyocardialfibrosisinspontaneouslyhypertensiverats.E