Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibraries(Rac)-LanicemineCat.No.:HY-108235BCASNo.:61890-25-3分?式:C??H??N?分?量:198.26作?靶點:iGluR作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存?式:Pureform-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(504.39mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM5.0439mL25.2194mL50.4388mL5mM1.0088mL5.0439mL10.0878mL10mM0.5044mL2.5219mL5.0439mL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，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.5mg/mL(12.61mM);Clearsolution此?案可獲得≥2.5mg/mL(12.61mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述2.體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。請依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(12.61mM);Clearsolution1/3此?案可獲得≥2.5mg/mL(12.61mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.5mg/mL(12.61mM);Clearsolution此?案可獲得≥2.5mg/mL(12.61mM，飽和度未知)的澄溶液，此?案不適?于實驗周期在半個?以上的實驗。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性(Rac)-Lanicemine((Rac)-AZD6765)Lanicemine的外消旋體。Lanicemine(AZD6765)?種低捕獲的NMDA受體拮抗劑，Ki為0.56-2.1μM。CHO和?蟾母細胞中，IC50分別為4-7μM和6.4μM。具有抗抑郁作?[1]。IC50&TargetNMDAreceptor[1]體內(nèi)研究Lanicemineproducessustainedantidepressantefficacywithminimalpsychotomimeticadverseeffects[1].Lanicemine(3,10or30?mg/kg;intraperitoneal)notonlyengagesbraincircuitsinvolvedinthegenerationofgamma-electroencephalography(EEG),butalsoinfluencesthesenetworksindependentofthebroadersystems-leveldisruptionstypicalofketamine[1].AnimalModel:MaleSprague-Dawleyrats[1]Dosage:3,10or30?mg/kgAdministration:IntraperitonealResult:Producedpronounceddose-dependentelevationsinspontaneousgamma-bandEEG,butonlygammachangesforKetamineweretightlycoupledtoincreasesinlocomotoractivity.REFERENCES[1].SanacoraG,etal.Lanicemine:alow-trappingNMDAchannelblockerproducessustainedantidepressantefficacywithminimalpsychotomimeticadverseeffects.MolPsychiatry.2014Sep;19(9):978-85.McePdfHeight2/3MedChemExpress(MCE)只為有資