Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDMCMhydrochlorideCat.No.:HY-100369ACASNo.:1215833-62-7分?式:C??H??ClN?O?分?量:350.8作?靶點(diǎn):GABAReceptor作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存?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:25mg/mL(71.27mM;Needultrasonic)DMSO:10mg/mL(28.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8506mL14.2531mL28.5063mL5mM0.5701mL2.8506mL5.7013mL10mM0.2851mL1.4253mL2.8506mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?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(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)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%salineSolubility:≥1mg/mL(2.85mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥1mg/mL(2.85mM);ClearsolutionBIOLOGICALACTIVITY?物活性DMCMhydrochloride?種苯?氮雜(benzodiazepine)?選擇性全反向激動劑。DMCM對?重組GABAAαxβ3γ2受體亞型具有親和?，對α1，α2，α3和α5受體的Ki值分別為10nM，13nM，7.5nM，2.2nM[1]。IC50&TargetKi:10nM(GABAAα1?receptor),13nM(GABAAα2receptor),7.5nM(GABAAα3?receptor),2.2nM(GABAAα5?receptor)[1]體內(nèi)研究DMCMhaspotentconvulsant,proconvulsantandanxiogenicpropertiesinvivo.DMCM(20-60mg/kg;i.p.)producesmodestanxiolytic-likeeffectsinγ2I77mice[2].AnimalModel:Maleγ2I77mice[2]Dosage:20mg/kgand60mg/kgAdministration:Injectedi.p.Result:Producedmodestanxiolytic-likeeffects.REFERENCES[1].ChambersMS,etal.Anorallybioavailable,functionallyselectiveinverseagonistatthebenzodiazepinesiteofGABAAalpha5receptorswithcognitionenhancingproperties.JMedChem.2004Nov18;47(24):5829-32.[2].Lepp?E,etal.Agonisticeffectsofthebeta-carbolineDMCMrevealedinGABA(A)receptorgamma2subunitF77Ipoint-mutatedmice.Neuropharmacology.2005Mar;48(4):469-78.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchus