Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELadostigilhemitartrateCat.No.:HY-10400CASNo.:209394-46-7Synonyms:TV-3326hemitartrate分?式:C??H??N?O?.?/?C?H?O?分?量:694.77作?靶點:MonoamineOxidase;AChE作?通路:NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:50mg/mL(71.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.4393mL7.1966mL14.3933mL5mM0.2879mL1.4393mL2.8787mL10mM0.1439mL0.7197mL1.4393mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥1.25mg/mL(1.80mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.25mg/mL(1.80mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(1.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性Ladostigil(TV-3326)hemitartrate?種?服有效的膽堿酯酶(cholinesterase)和腦選擇性單胺氧化酶(MAO)的雙重抑制劑，抑制MAO-B和AChE的IC50值分別為37.1和31.8μM。Ladostigilhemitartrate具有神經保護，抗氧化和抗炎作?，可?于抑郁癥和阿爾茨海默癥的研究。IC50&TargetMAO-BAChE37.1nM(IC50)31.8nM(IC50)體外研究Ladostigil(1-10μM)hemitartrateexertsneuroprotectiveactivities,includingapreventionofthefallofthemitochondrialmembranepotential(ψ),attenuationofapoptoticcascadesandaninhibitionofROSproductioninducedbyOSinsults[2].Ladostigil(1-10μM)hemitartratehasasignificantneuroprotectiveactivity,includinginhibitionofcaspase-3activation,inductionofBcl-2andreductionofBadandBaxgeneandproteinexpressioninhumanneuroblastomaSK-N-SHcells[2].體內研究Ladostigil(17mg/kg;p.o.dailyfor6weeks)hemitartrateabolishestheirhyperanxietyanddepressive-likebehaviourintheelevatedplusmaze(EPM)andforcedswimtests(FST)testsinadulthoodfrompubertytoprenatally-stressedrats[4].Ladostigil(50μmol/kg;singlep.o.)hemitartraterestoresthelossofepisodicmemoryintheobjectrecognitiontestinrats[3].AnimalModel:Pathogen-free(SPF)Sprague-Dawleyrats[4]Dosage:17mg/kgAdministration:P.o.(addedtothedrinkingwater)dailyfor6weeksResult:InhibitedbrainMAO-AandBbymorethan60%.Reducedhyperanxietyofmaleandfemaleprenatallystressed(PS)ratsintheEPManddepressive-likebehaviourintheFST.REFERENCES[1].DenyaI,et,al.Design,synthesisandevaluationofindolederivativesasmultifunctionalagentsagainstAlzheimer'sdisease.Medchemcomm.2018Jan16;9(2):357-370.[2].WeinrebO,et,al.Ladostigil:anovelmultimodalneuroprotectivedrugwithcholinesteraseandbrain-selectivemonoamineoxidase2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEinhibitoryactivitiesforAlzheimer'sdiseasetreatment.CurrDrugTargets.2012Apr;13(4):483-94.[3].WeinstockM,et,al.Ladostigil,anovelmultifunctionaldrugforthetreatmentofdementiaco-morbidwithdepression.JNeuralTransmSuppl.2006;(70):443-6.[4].PoltyrevT,et,al.Effectofchronictreatmentwithladostigil(TV-3326)onanxiogenicanddepressive-likebehaviourandonactivityofthehypothalamic-pituitary-adrenalaxisinmaleandfemaleprenatallystressedrats.Psychopharmacology(Berl).2005Aug;181(1):118-25.McePdfHeightCaution:Producthas