3-MethyladenineisaselectivePI3KinhibitorwithIC50of25μMand60μMforVps34andPI3Kγ,respectively,anditcaninhibitallPtdIns3Ksat10mM.CustomerValidation•JDermatolSci.2017Oct11.•BiochemBiophysResCommun.2016Dec2;481(1-2):90-96.Description3-MethyladenineisaselectivePI3KinhibitorwithIC50of25μMand60μMforVps34andPI3Kγ,respectively,anditcaninhibitallPtdIns3Ksat10mM.IC50&TargetIC50:25μM(Vps34),60μM(PI3Kγ)InVitro3-methyladenineshowssomelimitedVps34preferenceinvitro,withanIC50of25µMforVps34ascomparedwith60µMforPtdIns3Kγ,and3-methyladenine(10mM)caninhibitallPtdIns3Ks[1].3-methyladenine(3-MA,5mM)suppressesautophagyinHeLacellsunderbothglucose-freeconditionsandnormalconditions.3-methyladenineinducescaspase-dependentcelldeathinHeLacells,andthedeathoccursindependentlyoftheinhibitionofautophagy.3-MA(1mM)significantlyshortensthedurationofnocodazole-induced-prometaphasearrest[2].Alargenumberofneuronsfromthe3-MAgroupareintheearlystageofapoptosis,displayingcellshrinkage,nuclearandchromatincondensationandaggregationattheedgeofthenucleus[3].InVivo3-methyladenine-treatmentsignificantlyaggravatesneurologicalsymptomsandapoptoticcelldeathafterSAH[3].References[1].MillerS,etal.FindingafittingshoeforCinderella:searchingforanautophagyinhibitor.Autophagy.2010Aug;6(6):805-807.[2].HouH,etal.Inhibitorsofphosphatidylinositol3"-kinasespromotemitoticcelldeathinHeLacells.PLoSOne.2012;7(4):e35665.[3].JingCH,etal.Autophagyactivationisassociatedwithneuroprotectionagainstapoptosisviaamitochondrialpathwayinaratmodelofsubarachnoidhemorrhage.Neuroscience.2012Jun28;213:144-153.PreparingStockSolutionsConcentrationVolumeMass1mg5mg10mg1mM6.7047mL33.5233mL67.0466mL5mM1.3409mL6.7047mL13.4093mL10mM0.6705mL3.3523mL6.7047mLPleaserefertothesolubilityinformationtoselecttheappropriatesolvent.CellAssay[2]CellviABIlityisdeterminedbyatrypanblueexclusionassay.Cellsareculturedinthemediumwith3-Methyladenine.BothadherentandfloatingcellsarecollectedandsUSPendedinphosphatebufferedsaline(PBS,pH7.4)atafinaldensityof1-2×106/mL.Anequalvolumeof0.4%trypanbluesolution(w/v,inPBS)isaddedtothecellsuspensionandmixedthoroughly.Afterincubationatroomtemperaturefor3min,cellcountingisperformedusingahemacytometer.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalAdmiNISTration[3]3-Methyladenineisdissolvedinnormalsaline.Animalsarepositionedinastereotacticframeandtreatedwith5-μLintracerebralventricularinjectionsofautophagyinducerRAP(20 pmol),inhibitor3-Methyladenine(3-MA,400 nmol)orvehicle20 minbeforeSAHonset.Intracerebralventricularinjectionsaremadeintotheright lateralventricle atcoordinatesof0.8 mmanteriortoposteriorbregma,1.5 mmmidtolateral,3.8 mmdorsaltoventral.Aftertheinjection,thesyringeisleftinthesitefor30 sbeforeremoval,andtheburrholeisfilledwathbonewax.Drugdosesareselectedonthebasisofpreviouspublishedstudiesandpilotexperimentsinourlaboratory.3-MAisdissolvedinnormalsalinebyheatingthesolutionto60-70°Cimmediatelybeforetreatment.RAPisfirstdissolvedinethanolandthendilutedwithnormalsaline(finalethanolconcentrationReferences[1].MillerS,etal.FindingafittingshoeforCinderella:searchingforanautophagyinhibitor.Autophagy.2010Aug;6(6):805-807.[2].HouH,etal.Inhibitorsofphosphatidylinositol3"-kinasespromotemitoticcelldeathinHeLacells.PLoSOne.2012;7(4):e35665.[3].JingCH,etal.Autophagyactivationisassociatedwithneuroprotectionagainstapoptosisviaamitochondrialpathwayinaratmodelofsubarachnoidhemorrhage.Neuroscience.2012Jun28;213:144-153.MolecularWeight149.15FormulaC₆H₇N₅CASNo.5142-23-4StoragePowder-20°C3years 4°C2yearsInsolvent-80°C6months -20°C1monthShippingRoomtemperatureincontinentalUS;mayvaryelsewhereSolvent&SolubilityDMSO:≥1.5mg/mL;DMSO:6.8mg/mL(Needultrasonic);H2O:8.82mg/mL(Needultrasonic)*"

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