Methotrexate-Amethopterin-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMethotrexateCat.No.:HY-14519CASNo.:59-05-2Synonyms:Amethopterin;CL14377;WR19039分?式:C??H??N?O?分?量:454.44作?靶點(diǎn):Antifolate;DNA/RNASynthesis;ADCCytotoxin;Apoptosis;Bacterial作?通路:CellCycle/DNADamage;Antibody-drugConjugate/ADCRelated;Apoptosis;Anti-infection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(110.03mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2005mL11.0026mL22.0051mL5mM0.4401mL2.2005mL4.4010mL10mM0.2201mL1.1003mL2.2005mL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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.50mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.50mM);Clearsolution3.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(5.50mM);Clearsolution4.請(qǐng)依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.50mM);ClearsolutionBIOLOGICALACTIVITY?物活性Methotrexate(Amethopterin)?種抗代謝(antimetabolite)和抗葉酸劑(antifolate)，可抑制?氫葉酸還原酶，從?防?葉酸轉(zhuǎn)化為四氫葉酸并抑制DNA合成。Methotrexate也?種免疫抑制劑和抗腫瘤劑，?于類風(fēng)濕關(guān)節(jié)炎和研究多種癌癥(如急性淋巴細(xì)胞??病)。IC50&TargetTraditionalCytotoxicAgents體內(nèi)研究Methotrexate(Amethopterin)reducesthymusandspleenindicesofmice.Methotrexatemarkedlydecreaseswhitebloodcells,thymicandspleniclymphocytesatdose≥5mg/kg.However,thereisasignificantdifferencebetweenthetreatmentpluscontrolgroupandthemodelgroup(p[2].Methotrexate(MTX)(2mg/kg;i.p.;onceinaweekfor5weeks)iseffectiveinFreund'scompleteadjuvant-inducedarthritis.ThecombinationofMethotrexate(1mg/kg;i.p.;onceinaweekfor5weeks)andCurcumin(30mg/kgand100mg/kg,thriceaweekfor5weeks;i.p.)showsasignificantanti-arthriticactionandprotectionfromhematologicaltoxicity[4].PROTOCOLCellAssay[1]Eachcelllineisstudiedingrowthinhibitionexperimentsusing96-wellmicrotiterplates.Asantifolsarescheduledependent,preliminaryexperimentsareaimedatdefiningthelongestdurationofexposurethatwouldallowforcontinuouslogarithmicphasegrowthofcellswithoutchangingoftheculturemediawhilemaintainingalinearrelationshipbetweenSRBopticaldensityandcellnumber.Twenty-fourhoursaftercellplating,thecelllinesareexposedtotheantifolfor120h(threereplicatesperexperiment).Toensurethatacompletesigmoidalsurvival-concentrationcurvecouldbeobserved,thefollowingdrugconcentrationsarestudied:Methotrexate(0.002-5μM),AMT(0.0001-1μM),PXD(0.0003-10μM),TLX(0.0002-0.5μM).Experimentsarerepeatedatleasttwice[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[2]Administration[2]ThecombinationofbioactivephytochemicalsisadministeredoneweekpriortotheMethotrexateexposure.TreatmentgroupI:micearegivenacombinationofgreenteapolyphenolsandeleutherosidesfromSiberianginseng(0.2mL/10g,i.g.oncedaily)for15days,andasingledoseofMethotrexate(2mg/kg,i.p.oncedaily)isaddedonthe8thday.TreatmentgroupII:micearegivenacombinationofgrapeseed2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEproanthocyanidinsandeleutherosidesfromSiberianginsengfor15days,andMethotrexateisadministeredonthe8thdayinasimilarmanner.Modelgroup:animalsreceiveddistilledwaterinsteadofbioactivephytochemicalscombinationsfor15daysandthesameMethotrexateprotocolappliedtothisgrouponthe8thday.Controlgroup:micearegivendistilledwaterthrough15daysandphysiologicalsalineinsteadofMethotrexateisadministeredonthe8thdayinasimilarmanner.Twelvehoursafterthefinaldoses,theanimalsareeuthanizedbycervicaldislocation.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Small.2022Jul;18(30):e2202337.?EMBOMolMed.2022Feb17;e14552.?JPharmAnal.7August2022.?CellDeathDis.2020Nov12;11(11):976.?ActaPharmacolSin.2021Jan;42(1):108-114.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TianH,etal.Understandingthemechanismsofactionofmethotrexate:implicationsforthetreatmentofrheumatoidarthritis.BullNYUHospJtDis.2007;65(3):168-73.[2].SwierkotJ,etal.Methotrexateinrheumatoidarthritis.PharmacolRep.2006Jul-Aug;58(4):473-92.[3].EhabTousson,etal.TheEffectofL-carnitineonAmethopterin-inducedToxicityinRatLargeIntestine.[4].BanjiD,etal.EvaluationoftheconcomitantuseofmethotrexateandcurcuminonFreund'scompleteadjuvant-inducedarthritisandhematologicalin