Gabazine-SR95531-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGabazineCat.No.:HY-103533CASNo.:104104-50-9Synonyms:SR95531分⼦式:C₁₅H₁₈BrN₃O₃分⼦量:368.23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:100mg/mL(271.57mM;Needultrasonic)DMSO:≥75mg/mL(203.68mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7157mL13.5785mL27.1569mL5mM0.5431mL2.7157mL5.4314mL10mM0.2716mL1.3578mL2.7157mL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)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.79mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.79mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.79mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GabazineGABAA受体的选择性竞争性拮抗剂，其对GABA受体的IC50值为~0.2μM。IC50&Target0.2μM(GABAreceptor)[1].体外研究BothbicucullineandGabazine(SR95531)havebeencharacterizedascompetitiveinhibitorsofGABAbindingtotheGABAAreceptor.GabazineismorepotentthanbicucullineatblockingcurrentselicitedbyGABA,withanIC50forcurrentselicitedby3μMGABAof~0.2μMandaHillcoefficientof1.0.Gabazinereducesthecurrentselicitedby10μMalphaxaloneby~30%,forresponsesofreceptorscontainingwildtypeβ2subunits.TheconcentrationofGabazinerequiresproducinghalfthemaximalblockis~0.2μM.Gabazinealsocouldonlyproduceapartialblockofcurrentsgatedby300μMpentobarbital.Themaximalreduction,again,is~30%,andtheconcentrationofGabazinerequiredtoproducehalfthemaximalblockis~0.15μM[1].户使⽤本产品发表的科研⽂献•OxidMedCellLongev.2022Apr15;2022:3716609.•Phytomedicine.2022Jan29;98:153965.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].UenoS,etal.BicucullineandgabazineareallostericinhibitorsofchannelopeningoftheGABAAreceptor.JNeurosci.1997Jan15;17(2):625-34.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.