Elenbecestat-E2609-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEElenbecestatCat.No.:HY-109055CASNo.:1388651-30-6Synonyms:E2609分?式:C??H??F?N?O?S分?量:437.44作?靶點(diǎn):Beta-secretase作?通路:NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥250mg/mL(571.51mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2860mL11.4301mL22.8603mL5mM0.4572mL2.2860mL4.5721mL10mM0.2286mL1.1430mL2.2860mL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。-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)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.75mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.75mM);ClearsolutionBIOLOGICALACTIVITY?物活性Elenbecestat(E2609)?種?效、有?服活性的，能透過(guò)CNS的BACE-1抑制劑。Elenbecestat有潛??于阿爾茨海默病(AD)的研究。IC50&TargetBACE-1[1]體外研究Elenbecestat(E2609)isapotentBACE1inhibitorwithanIC50of~7nmol/Lincell-basedassay[2].ElenbecestathasbeenshowntoreduceAbproductionintheplasma,brain,andcerebrospinalfluid(CSF)ofrodents[2].體內(nèi)研究Elenbecestat(E2609;0.3-30mg/kg;p.o.)potentlyinhibitsAb1-40andAb1-42productionintheplasmaandCSFofnon-humanprimates[2].Elenbecestatdisplaystheplasmahalf-lifeof12-16hoursafteroncedailydosing[1].AnimalModel:Cynomolgusmonkeys(Pharmacokineticanalysis)[2]Dosage:0.3mg/kg;1mg/kg;3mg/kg;30mg/kgAdministration:OraladministrationResult:PotentlyinhibitsAb1-40andAb1-42productionintheplasmaandCSF.REFERENCES[1].KumarD,etal.SecretaseinhibitorsforthetreatmentofAlzheimer'sdisease:Longroadahead.EurJMedChem.2018Mar25;148:436-452.[2].Asingledoseofthebeta-secretaseinhibitor,e2609,decreasesCSFbace1enzymaticactivityincynomolgusmonkeys.Alzheimer’s&Dementia,8(4),P224.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse