Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGabazineCat.No.:HY-103533CASNo.:104104-50-9Synonyms:SR95531分?式:C??H??BrN?O?分?量:368.23作?靶點: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)體外實驗H2O:100mg/mL(271.57mM;Needultrasonic)DMSO:≥75mg/mL(203.68mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7157mL13.5785mL27.1569mL5mM0.5431mL2.7157mL5.4314mL10mM0.2716mL1.3578mL2.7157mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?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：(為保證實驗結(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)實驗的?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)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.79mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.79mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.79mM);ClearsolutionBIOLOGICALACTIVITY?物活性GabazineGABAA受體的選擇性競爭性拮抗劑，其對GABA受體的IC50值為~0.2μM。IC50&Target0.2μM(GABAreceptor)[1].體外研究BothbicucullineandGabazine(SR95531)havebeencharacterizedascompetitiveinhibitorsofGABAbindingtotheGABAAreceptor.GabazineismorepotentthanbicucullineatblockingcurrentselicitedbyGABA,withanIC50forcurrentselicitedby3μMGABAof~0.2μMandaHillcoefficientof1.0.Gabazinereducesthecurrentselicitedby10μMalphaxaloneby~30%,forresponsesofreceptorscontainingwildtypeβ2subunits.TheconcentrationofGabazinerequiresproducinghalfthemaximalblockis~0.2μM.Gabazinealsocouldonlyproduceapartialblockofcurrentsgatedby300μMpentobarbital.Themaximalreduction,again,is~30%,andtheconcentrationofGabazinerequiredtoproducehalfthemaximalblockis~0.15μM[1].戶使?本產(chǎn)品發(fā)表的科研?獻?OxidMedCellLongev.2022Apr15;2022:3716609.?Phytomedicine.2022Jan29;98:153965.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].UenoS,etal.BicucullineandgabazineareallostericinhibitorsofchannelopeningoftheGABAAreceptor.JNeurosci.1997Jan15;17(2):625-34.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.