Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBlarcamesinehydrochlorideCat.No.:HY-101864CASNo.:195615-84-0分?式:C??H??ClNO分?量:317.85作?靶點(diǎn):SigmaReceptor作?通路:NeuronalSignaling儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:100mg/mL(314.61mM;Needultrasonic)DMSO:25mg/mL(78.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.1461mL15.7307mL31.4614mL5mM0.6292mL3.1461mL6.2923mL10mM0.3146mL1.5731mL3.1461mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.87mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(7.87mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.87mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:100mg/mL(314.61mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Blarcamesinehydrochloride?個(gè)Sigma-1受體激動(dòng)劑，其IC50值為860nM。IC50&TargetIC50:860nM(Sigma-1Receptor)[1]體內(nèi)研究Thepre-administrationofBlarcamesineleadstoadose-dependentattenuationofthescopolamineinducedalternationdeficit,significantat1and3mg/kg.Thepre-treatmentwithBlarcamesinehydrochlorideattenuatestheimpairmentsofstep-throughlatency,dosedependentlyandsignificantlyatdoseshigherthan0.3mg/kg[1].TheBlarcamesinehydrochloridetreatmentdose-dependentlyblockstherecognitionmemorydeficit,withasignificanteffectmeasuredat1?mg/kg.Onedayafterinjections,thesignificantAβ25-35-induceddecreaseinAktphosphorylationissignificantlyattenuatedbyBlarcamesinehydrochlorideat0.1and1?mg/kgdose.Sevendaysafterinjections,BlarcamesinehydrochlorideattenuatesthedecreaseinSer9phosphorylationinducedbythepeptideat0.3and1?mg/kg.TheBlarcamesinehydrochloridetreatmentdose-dependentlypreventstheAβ25-35-inducedincreaseinAβ1-42content,withasignificanteffectatthehighestdosetested[2].PROTOCOLAnimalMalemiceaged7-9weeksandweighing32±2?gareused.Drugs(includingBlarcamesinehydrochloride)areAdministration[2]broughtuptoeachdosebydilutionandinjectedinavolumeof100?μL/20?gbodyweight.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