Blarcamesine-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBlarcamesinehydrochlorideCat.No.:HY-101864CASNo.:195615-84-0分⼦式:C₁₉H₂₄ClNO分⼦量:317.85作⽤靶点:SigmaReceptor作⽤通路:NeuronalSignaling储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验H2O:100mg/mL(314.61mM;Needultrasonic)DMSO:25mg/mL(78.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1461mL15.7307mL31.4614mL5mM0.6292mL3.1461mL6.2923mL10mM0.3146mL1.5731mL3.1461mL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,awayfrommoisture)。-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%salineSolubility:≥2.5mg/mL(7.87mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(7.87mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.87mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:100mg/mL(314.61mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Blarcamesinehydrochloride⼀个Sigma-1受体激动剂，其IC50值为860nM。IC50&TargetIC50:860nM(Sigma-1Receptor)[1]体内研究Thepre-administrationofBlarcamesineleadstoadose-dependentattenuationofthescopolamineinducedalternationdeficit,significantat1and3mg/kg.Thepre-treatmentwithBlarcamesinehydrochlorideattenuatestheimpairmentsofstep-throughlatency,dosedependentlyandsignificantlyatdoseshigherthan0.3mg/kg[1].TheBlarcamesinehydrochloridetreatmentdose-dependentlyblockstherecognitionmemorydeficit,withasignificanteffectmeasuredat1ꢀmg/kg.Onedayafterinjections,thesignificantAβ25-35-induceddecreaseinAktphosphorylationissignificantlyattenuatedbyBlarcamesinehydrochlorideat0.1and1ꢀmg/kgdose.Sevendaysafterinjections,BlarcamesinehydrochlorideattenuatesthedecreaseinSer9phosphorylationinducedbythepeptideat0.3and1ꢀmg/kg.TheBlarcamesinehydrochloridetreatmentdose-dependentlypreventstheAβ25-35-inducedincreaseinAβ1-42content,withasignificanteffectatthehighestdosetested[2].PROTOCOLAnimalMalemiceaged7-9weeksandweighing32±2ꢀgareused.Drugs(includingBlarcamesinehydrochloride)areAdministration[2]broughtuptoeachdosebydilutionandinjectedinavolumeof100ꢀμL/20ꢀgbodyweight.Animalsareusedbetweendays1and9afteri.c.v.injectionsforbehavioraltestingorkilledbeforebiochemicalmeasures[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].VillardV,etal.Anti-amnesicandneuroprotectivepotentialsofthemixedmuscarinicreceptor/sigma1(σ1)ligandANAVEX2-73,anovelaminotetrahydrofuranderivative.JPsychopharmacol.2011Aug;25(8):1101-17.[2].ValentineLahmy,etal.BlockadeofTauHyperphosphorylationandAβ1-42GenerationbytheAminotetrahydrofuranDerivativeANAVEX2-73,aMixedMuscarinicandσ1ReceptorAgonist,inaNontransgenicMouseModelofAlzheimer'sDisease.NeuropsychopharmacologyMcePdfHeightCaution:Producthasnotbe