Lu-AF21934-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELuAF21934Cat.No.:HY-100366CASNo.:1445605-23-1分⼦式:C₁₄H₁₆Cl₂N₂O₂分⼦量:315.2作⽤靶点:mGluR作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥80mg/mL(253.81mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1726mL15.8629mL31.7259mL5mM0.6345mL3.1726mL6.3452mL10mM0.3173mL1.5863mL3.1726mL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。-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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(7.93mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.93mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.93mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LuAF21934选择性和脑渗透性的mGlu4受体正变构调节剂，对mGlu4受体的EC50为500[1]。IC50&TargetmGlu4Receptor500nM(EC50)体内研究LuAF21934treatmentshowsadose-dependentanxiolytic-likeeffectinthestress-inducedhyperthermia,four-plate,andmarble-buryingtests.Theanti-hyperthermiceffectofLuAF21934(5mg/kg)intheSIHtestisinhibitedbythebenzodiazepinereceptorantagonistflumazenil(10mg/kg)andisnotserotonindependent.LuAF21934doesnotproduceantidepressant-likeeffectsinthetailsuspensiontestinmice;however,itdecreasesthebasallocomotoractivityofmicethatarenothabituatedtoactivitycages[1].LuAF21934(0.5-5mg/kgsc)doesnotinfluencetremorbutatdosesof0.5and2.5mg/kgreversesharmaline-inducedhyperactivity.LuAF21934atadoseof2.5mg/kgpotentiatestheinhibitoryinfluenceofharmalineontheexploratoryactivityandAP1duringthefirst30minofthemeasurementandcounteractstheharmaline-increasedbasicactivityduringtheperiodof30-90min[2].LuAF21934(0.1-5mg/kg)dose-dependentlyinhibitshyperactivityinducedbyMK-801oramphetamine.Italsoantagonizesheadtwitchesandincreasesfrequencyofspontaneousexcitatorypostsynapticcurrentsinbrainslices,inducedbyDOI[3].PROTOCOLAnimalRats:LuAF21934isdispersedin20%(2-hydropropyl)-b-cyclodextrinandareadministeredsubcutaneouslyAdministration[1](s.c.)60minbeforethetest.LuAF21934(2,5,10and15mg/kg,s.c.)anddiazepam(5mg/kg,i.p.)areadministeredacutely1hbeforetheVogel’sconflicttest.Theeffectsofeachdruginallexperimentsaremeasuredingroupsof8-10animals[1].Mice:LuAF21934isdispersedin20%(2-hydropropyl)-b-cyclodextrinandareadministeredsubcutaneously(s.c.)60minbeforethetest.Micearegentlyplacedintotheboxandallowedtoexplorefor15s.Then,eachtimeamousepassedfromoneplatetoanother,theexperimenterelectrifiesthewholefloorthusevokingavisibleflightreactionoftheanimal.Iftheanimalcontinuesrunning,nonewshockisdeliveredforthefollowing3s[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].AnnaSławińska,etal.Anxiolytic-butnotantidepressant-likeactivityofLuAF21934,anovel,selectivepositiveallostericmodulatorofthemGlu?receptor.Neuropharmacology.2013Mar;66:225-35.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[2].OssowskaK,etal.LuAF21934,apositiveallostericmodulatorofmGlu4receptors,reducestheharmaline-inducedhyperactivitybutnottremorinrats.Neuropharmacology.2014Aug;83:28-35.[3].AnnaSławińska,etal.Theantipsychotic-likeeffectsofpositiveallostericmodulatorsofmetabotropicglutamatemGlu4receptorsinrodents.BrJPharmacol.2013Aug;169(8):1824-39.McePdfHe