Chlorpromazine-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEChlorpromazineCat.No.:HY-12708CASNo.:50-53-3分?式:C??H??ClN?S分?量:318.86作?靶點(diǎn):DopamineReceptor;CytochromeP450;Autophagy作?通路:GPCR/GProtein;NeuronalSignaling;MetabolicEnzyme/Protease;Autophagy儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Chlorpromazine可?于抗精神病的研究，可?擾多個(gè)配體和電壓門控通道[1]。Chlorpromazine?種有效的多巴胺(dopamine)拮抗劑[2]。Chlorpromazine抑制CYP1A2和CYP2D6活性，IC50分別為9.5和20μM[3]。Chlorpromazine可誘導(dǎo)?噬(autophagy)，但不誘導(dǎo)細(xì)胞凋亡[4]。體外研究TheeffectofChlorpromazineonGABAARbindingrate,resultinginsloweronsetofGABA-evokedcurrents,providesatooltoestimatethespeedofsynapticclearanceofGABA.Chlorpromazine,awidelyusedantipsychoticdrug,stronglyaffectstheGABA-mediatedinhibitorysynaptictransmissionbydecreasingtheamplitudeandbyacceleratingthedecayofmIPSCs.CPZdecreasestheamplitudeandacceleratesthedecayofmIPSCs[1].ChlorpromazineinhibitsCYP1A2andCYP2D6activitywithKisof4.75and10μM,respectively[3].Chlorpromazineisaphenothiazinederivativebelongingtothefirstgenerationofatypicalantipsychoticagent.Chlorpromazine(10-40μM)showsantitumoreffectsinU-87MGgliomacells.Chlorpromazinepromotesantitumoralactionthroughinductionofcelldeath[4].Chlorpromazine(20μM)causesinhibitionofcellcycleprogression[4].CellProliferationAssay[4]CellLine:U-87MGgliomacellsConcentration:0,10,20and40μMIncubationTime:0,24and48hours1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Adecreaseincellularproliferationwasobservedincellsinadose-andtime-dependentmannercomparedwithuntreatedcontrolcells.Asignificantdecreaseincellviabilitywasobservedincellstreatedfor24hwithhighconcentration(≥20μM)comparedwithuntreatedcontrolcells.WesternBlotAnalysis[4]CellLine:U-87MGcellsConcentration:20μMIncubationTime:0,12,24,48hoursResult:After12hexposure,thelevelsofcyclinAandcyclinB1decreased,whereaslevelsofcyclinD1,proliferatingcellnuclearantigenandGAPDHremainedunchanged.體內(nèi)研究Chlorpromazine(20mg/kg;injectedintraperitoneallydailyfor7days)inhibitsxenografttumorgrowthinnudemouse[4].AnimalModel:5-to6-week-oldathymicnudemicebearingintracranialU-87MGxenografttumors[4]Dosage:20mg/kgAdministration:Injectedintraperitoneallydailyfor7daysResult:Treatmentinhibitedxenografttumorgrowthonday24comparedwithcontroltreatment.Inhibitionoftumorgrowthbegantobeobservedafterday17;onday24,thetumorsizesignificantlydecreasedfrom690±112mm3inthecontrolgroupto390±81mm3inthetreatedgroup,accountingfora43.5%inhibitionintumorgrowth.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?AdvFunctMater.2020,2004940.?ACSNano.2020Nov24;14(11):14698-14714.?JAmChemSoc.2018Dec12;140(49):17234-17240.?Biomaterials.13January2022,121373.?Theranostics.2021May24;11(15):7308-7321.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].JWMozrzymas,etal.ChlorpromazineinhibitsminiatureGABAergiccurrentsbyreducingthebindingandbyincreasingtheunbinding2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemErateofGABAAreceptors.JNeurosci.1999Apr1;19(7):2474-88.[2].MWHarrold,etal.Chargedanaloguesofchlorpromazineasdopamineantagonists.JMedChem.1987Sep;30(9):1631-5.[3].GuillermoGervasini,etal.Comparativecytochromep450invitroinhibitionbyatypicalantipsychoticdrugs.ISRNPharmacol.2013;2013:792456.[4].SoonYoungShin,etal.TheantipsychoticagentchlorpromazineinducesautophagiccelldeathbyinhibitingtheAkt/mTORpathwayinhumanU-87MGgliomacells.Carcinogenesis.2013Sep;34(9):2080-9.McePdfHeightCaution