Amodiaquine-dihydrochloride-dihydrate-Amodiaquin-dihydrochloride-dihydrate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAmodiaquinedihydrochloridedihydrateCat.No.:HY-B1322CASNo.:6398-98-7Synonyms:Amodiaquindihydrochloridedihydrate分⼦式:C₂₀H₂₂ClN₃O.₂H₂O.₂HCl分⼦量:464.81作⽤靶点:Parasite;HistoneMethyltransferase作⽤通路:Anti-infection;Epigenetics储存⽅式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验DMSO:100mg/mL(215.14mM;Needultrasonic)H2O:20mg/mL(43.03mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1514mL10.7571mL21.5142mL5mM0.4303mL2.1514mL4.3028mL10mM0.2151mL1.0757mL2.1514mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.38mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.38mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Amodiaquinedihydrochloridedihydrate(Amodiaquindihydrochloridedihydrate)⼀种4-氨喹啉类抗疟剂，⼀种有效的具有⼝服活性的组胺N-甲转移酶(histamineN-methyltransferase)抑制剂。Amodiaquinedihydrochloridedihydrate也⼀种Nurr1激动剂，可特异性结合Nurr1的配体结合域，EC50为~20μM。抗炎作⽤。IC50&TargetEC50:~20μM(Nurr1-LBD(ligandbindingdomain))[1]HistamineN-methyltransferase[3]体外研究Amodiaquine(10-20μM;4hours)treatmentsuppressesLPS-inducedexpressionofproinflammatorycytokines(IL-1β,interleukin-6,TNF-αandiNOS)inadose-dependentmanner[1].Amodiaquine(5μM;24hours)significantlyinhibitsneurotoxin(6-OHDA-inducedcelldeathinprimarydopaminecellsasexaminedbythenumberofTH+neuronsanddopamineuptake.TheneuroprotectiveeffectofAmodiaquineisalsoobservedinratPC12cells[1].RT-PCR[1]CellLine:PrimarymicrogliaConcentration:10µM,15µM,20µMIncubationTime:4hoursResult:SuppressedLPS-inducedexpressionofproinflammatorycytokines(IL-1β,interleukin-6,TNF-αandiNOS)inadose-dependentmanner.体内研究Amodiaquine(40mg/kg;intraperitonealinjection;daily;for3days;maleICRmice)treatmentdiminishesperihematomalactivationofmicroglia/macrophagesandastrocytes.AmodiaquinealsosuppressesICH-inducedmRNAexpressionofIL-1β,CCL2andCXCL2,andamelioratedmotordysfunctionofmice[2].AnimalModel:MaleICRmice(8-10ꢀweeksofage)inducedntracerebralhemorrhage(ICH)[2]Dosage:40mg/kgAdministration:Intraperitonealinjection;daily;for3daysResult:Diminishedperihematomalactivationofmicroglia/macrophagesandastrocytes.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•CellRep.2021Apr6;35(1):108959.•OxidMedCellLongev.2021Feb10.•MetabBrainDis.2021Jan28.•BiochemBiophysResCommun.2020Feb19;522(4):862-868.•BiolPharmBull.2022Feb3.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Chun-HyungKim,etal.NuclearreceptorNurr1agonistsenhanceitsdualfunctionsandimprovebehavioraldeficitsinananimalmodelofParkinson'sdisease.ProcNatlAcadSciUSA.2015Jul14;112(28):8756-61.[2].KeitaKinoshita,etal.ANurr1agonistamodiaquineattenuatesinflammatoryeventsandneurologicaldeficitsinamousemodelofintracerebralhemorrhage.JNeuroimmunol.2019May15;330:48-54.[3].AkiraYokoyama,etal.Effectofamodiaquine,ahistamineN-methyltransferaseinhibitor,on,Propionibacteriumacnesandlipopolysaccharide-inducedhepatitisinmice.EurJPharmacol.2007Mar8;558(1-3):179-84.[4].MTHOEKENGA.Thetreatmentofacutemalariawithsingleoraldosesofamodiaquin,chloroquine,hydroxychloroquineandpyrimethamine.AmJTropMedHyg.1954Sep;3(5):833-8.McePdfH