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

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDMCMhydrochlorideCat.No.:HY-100369ACASNo.:1215833-62-7分⼦式:C₁₇H₁₉ClN₂O₄分⼦量:350.8作⽤靶点:GABAReceptor作⽤通路:MembraneTransporter/IonChannel;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:25mg/mL(71.27mM;Needultrasonic)DMSO:10mg/mL(28.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8506mL14.2531mL28.5063mL5mM0.5701mL2.8506mL5.7013mL10mM0.2851mL1.4253mL2.8506mL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:≥1mg/mL(2.85mM);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:≥1mg/mL(2.85mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性DMCMhydrochloride⼀种苯⼆氮杂(benzodiazepine)⾮选择性全反向激动剂。DMCM对⼈重组GABAAαxβ3γ2受体亚型具有亲和⼒，对α1，α2，α3和α5受体的Ki值分别为10nM，13nM，7.5nM，2.2nM[1]。IC50&TargetKi:10nM(GABAAα1ꢀreceptor),13nM(GABAAα2receptor),7.5nM(GABAAα3ꢀreceptor),2.2nM(GABAAα5ꢀreceptor)[1]体内研究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].LeppäE,etal.Agonisticeffectsofthebeta-carbolineDMCMrevealedinGABA(A)receptorgamma2subunitF77Ipoint-mutatedmice.Neuropharmacology.2005Mar;48(4):469-78.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchus