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Medchemexpress/U0126(Synonyms: U0126-EtOH)/HY-12031/10mM*1mL in DMSO
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U0126isanon-ATPcompetitiveMEKinhibitor,withIC50of70nMand60nMforMEK1andMEK2,respectively.CustomerValidation•FrontImmunol.2017Oct10;8:1278.•CancerLett.2017Feb16;393:22-32.•JMolCellCardiol.2015Dec;89(PtB):268-79.•FreeRADIcBiolMed.2017Jul9;112:49-59.•Oncotarget.2017May16;8(20):33807-33826.•FrontMolNeurosci.2017Mar13;10:51.•OxidMedCellLongev.2017;2017:7426458.•OxidMedCellLongev.2017;2017:6175841.•CellSignal.2017Jan16;32:48-58. •CellSignal.2016Feb;28(2):81-93.•ACSChemNeurosci.2015Jan21;6(1):130-7.•CellCycle.2017Apr3;16(7):714-722.•Peptides.2016Oct14;86:72-79.•IntJMolMed.2017Jul;40(1):164-174.•IntJClinExpPathol.2017;10(7):7466-7474•EnvironSciPollutResInt.2017Jul10.•ThirdMilitaryMedicalUniversityDescriptionU0126isanon-ATPcompetitiveMEKinhibitor,withIC50of70nMand60nMforMEK1andMEK2,respectively.IC50&TargetIC50:70/60nM(MEK1/2)[1]InVitroTreatmentwithU0126efficientlyreducesProgenyvirustitersofalltestedstrainsinA549cells.WhilenMconcentrationsofU0126areefficienttoreduceH1N1vandH5N1(MB1),μMconcentrationsofU0126arerequiredtoreducethevirustiterofH5N1(GSB)andH7N7.TheEC50valuesforU0126againstH1N1vare1.2±0.4μMinA549cellsand74.7±1.0μMinMDCKIIcells[2].Rathepatocarcinomacells(FAO)stimulatedbyfetalcalfserum(FCS)exhibitsasignificantproportioninSphase(32.62%)whereasU0126stronglydecreasestheproportionofcellsinSphase(9.92%)andincreasestheproportionofcellsinG0-G1phaseandtoalesserextentinG2/M[3].InVivoMicearetreateddailywithU0126(i.p.,10.5mg/kg).Incontrolexperiment,tumorsizesareconstantorslightlyincreasealloverthekinetic.Attheopposite,inallU0126experiments,engraftmentandearlytumorgrowtharesignificantlydecreased.FurThermore,a60-70%reductioninthevolumeoftumorstreatedwithU0126isobtained9daysafterinjectionandthereafter[3].Ratsaresubjectedto120?minutestransientmiddlecerebralarteryocclusion(tMCAO)andthereaftertreatedwiththeU0126(i.p.,30mg/kg)at0and24hoursofreperfusion.AftertreatmentwithU0126,thevasoconstrictiontoS6cismarkedlyreduced[4].References[1].DunciaJV,etal.MEKinhibitors:thechemistryandBIOLOGicalactivityofU0126,itsanalogs,andcyclizationproducts.BioorgMedChemLett.1998,8(20),2839-2844.[2].DroebnerK,etal.AntiviralactivityoftheMEK-inhibitorU0126againstpandemicH1N1vandhighlypathogenicavianinfluenzavirusinvitroandinvivo.AntiviralRes.2011,92(2),195-203.[3].BessardA,etal.RNAi-mediatedERK2knockdowninhibitsgrowthoftumorcellsinvitroandinvivo.Oncogene.2008Sep11;27(40):5315-25.[4].AhnstedtH,etal.U0126attenuatescerebralvasoconstrictionandimproveslong-termneurologicoutcomeafterstrokeinfemalerats.JCerebBloodFlowMetab.2015Mar;35(3):454-60.PreparingStockSolutionsConcentrationVolumeMass1mg5mg10mg1mM2.3443mL11.7217mL23.4434mL5mM0.4689mL2.3443mL4.6887mL10mM0.2344mL1.1722mL2.3443mLPleaserefertothesolubilityinformationtoselecttheappropriatesolvent.CellAssay[2]U0126isdissolvedinDMSO(10mM)andstored,andthendilutedwithappropriatemedia(DMSO1%)beforeuse[2].A549andMDCKIIcellsareseededin96-wellcultureplatesatadensityof8×104cellsperwellinminimalessentialmedium(MEM)containing10%heat-inactivatedfetalcalfserum(FCS),100U/mLPenicillin,100mg/mLStreptomycin.Cellsareincubatedat37°Cwith5%CO2overnight.Thereafter,cellsarewashedtwicewithPBS.MEMcontainingdifferentconcentrationsofU0126(0.001-1000μM)isaddedtothecells.AfteradditionofU0126,cellsareincubatedfurtherfor48hat37°Cand5%CO2.Then,cellsarefixedbyincubationfor30minat4°Cwith100μL4%paraformaldehyde(PFA).Adding100μLcrystalvioletfor30minatroomtemperaturestainedviablecells.Afterstaining,platesarewashedanddried.Fortheextractionofcrystalvioletfromviablecells100μLof100%methanolisaddedtoeachwell.Afterincubationfor30minatroomtemperature,theextinctionismeasuredwithanenzyme-linkedimmunosorbentassay(ELISA)readeratOD=490nm.ThepercentageofcellviABIlityaftertreatmentwiththeantiviralcompoundiscalculated[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalAdmiNISTration[3][4]U0126isdissolvedinDMSO.Mice[3]Athymicfemalenudemice(SWISS,nu/nu)areused.Priortoinjection,FIcellsarelabeledwithastablefluorescentdyemolecule,DiAat10μg/mLfor5hat37°C.AfterwashingtoremovefreeDiA,cellsaretrypsinizedforinoculation(U0126experiments)ortransfection(RNAiexperiments).Biliaryepithelialcellsareinjectedsubcutaneously,attheindicatedtimes,intothetibiaofnudemice.Inthechemicalexperiments,3hafterinoculation,micearetreatedwithU0126(10.5mg/kg)dailybyintraperitonealinjection.Thelengthandwidthofeachtumoraremeasuredeverydaybyusingacaliper.Thefollowingformulaisusedtocalculatetumorvolumes=width2×length/2.Micearekilledattheendofexperiment.Tumorsareimmediatelyfrozeninliquidnitrogen.Rat[4]Twelve-week-oldfemaleWistarrats(250to265g)areusedU0126(30mg/kgintraperitoneally)isinjectedat0and24hoursofreperfusionaftertMCAObasedonthepreviousevaluationofthedruginmalerats.AnimalsinstudyIIareadministeredU0126orvehicleandarekilled14daysaftertMCAO.Experimentalgroupassignmentsarerandomizedandblindedtothesurgicalexperimenter.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.References[1].DunciaJV,etal.MEKinhibitors:thechemistryandbiologicalactivityofU0126,itsanalogs,andcyclizationproducts.BioorgMedChemLett.1998,8(20),2839-2844.[2].DroebnerK,etal.AntiviralactivityoftheMEK-inhibitorU0126againstpandemicH1N1vandhighlypathogenicavianinfluenzavirusinvitroandinvivo.AntiviralRes.2011,92(2),195-203.[3].BessardA,etal.RNAi-mediatedERK2knockdowninhibitsgrowthoftumorcellsinvitroandinvivo.Oncogene.2008Sep11;27(40):5315-25.[4].AhnstedtH,etal.U0126attenuatescerebralvasoconstrictionandimproveslong-termneurologicoutcomeafterstrokeinfemalerats.JCerebBloodFlowMetab.2015Mar;35(3):454-60.MolecularWeight426.56FormulaC₂₀H₂₂N₆OS₂CASNo.1173097-76-1StoragePowder-20°C3years 4°C2yearsInsolvent-80°C6months -20°C1monthShippingRoomtemperatureincontinentalUS;mayvaryelsewhereSolvent&SolubilityDMSO:≥49mg/mL*"
托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-Tropanylindole-3-carboxylate;lαH,5Αh-Tropan-3α-ylindole-3-carboxylate中文名称:托烷司琼中文同义词:托普西隆;托普西龙;曲匹西龙;托烷司琼;Β-托烷司琼;CS-348;Β-内托烷司琼;吲哚-3-甲酰氯;Β-托烷司琼(光学异构体);Β-托烷司琼,托烷司琼异构体CBNumber:CB3236404分子式:C17H20N2O2分子量:284.35MOLFile:89565-68-4.mol化学性质安全信息用途供应商112化学性质安全信息用途供应商112托烷司琼化学性质熔点:201-202°C沸点:448.5±35.0°C(Predicted)密度:1.26储存条件:2-8°C溶解度:H2O:soluble形态:solid酸度系数(pKa):15.38±0.30(Predicted)颜色:whiteCAS数据库:Chemicalbook89565-68-4(CASDataBaseReference)安全信息WGKGermany:3托烷司琼化学药品说明书托烷司琼|药物应用信息托烷司琼性质、用途与生产工艺临床评价Sorbe等报道本品对含顺铂(剂量50~89mg/m2)化疗方案引起的急性呕吐完全控制率为63%。58例恶性肿瘤化疗所致恶心、呕吐者,应用托烷司琼或昂丹司琼8mg分别在同一病人前后2个化疗周期的第1d给药前30min静脉注射,并用地塞米松10mg静脉滴注。结果两药控制急性及迟发性恶心、呕吐的疗效基本相似,均可达81%~100%。本品对强致吐化疗药物顺铂的止吐疗效突出。药物相关作用饮食可略为延长本品的吸收。本品与利福平、苯巴比妥等肝酶诱导药同时使用,可加快代谢,故快代谢型者需增加剂量,慢者则不必。西咪替丁等肝酶抑制药对本品血药浓度无明显影响。适应症托烷司琼临床用于预防和治疗癌症化疗引起的恶心和呕吐。化学性质结晶,熔点201-202℃(二氯甲烷-乙酸乙酯)。单盐酸托烷司琼(TropisetronMonohydroehloride):C17H20N2O2?HCI。[105826-92-4]。熔点283-285℃(分解)。用途有高效性和选择性的5-HT3受体拮抗剂。用于化疗所致的呕吐。用途为5-羟色胺拮抗药生产方法托品醇(I)和酰氯(Ⅱ)反应,可得托烷司琼。托烷司琼上下游产品信息上游原料托品醇下游产品
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