UCPH-101-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEUCPH-101Cat.No.:HY-10914CASNo.:1118460-77-7分?式:C??H??N?O?分?量:422.48作?靶點:Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥50mg/mL(118.35mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3670mL11.8349mL23.6698mL5mM0.4734mL2.3670mL4.7340mL10mM0.2367mL1.1835mL2.3670mL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。-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?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%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.92mM);ClearsolutionBIOLOGICALACTIVITY?物活性UCPH-101興奮性氨酸轉(zhuǎn)運?亞型1(EAAT1)的抑制劑，其IC50值為0.66μM。IC50&TargetIC50:0.66μM(EAAT1)[1]體外研究UCPH-101andUCPH-102inhibitEAAT1anioncurrentsinaconcentration-dependentmanner,withKDvaluesof0.34±0.03μM(Hill=1.3±0.13,n≥9)forUCPH-101and0.17±0.02μM(Hill=0.97±0.11,n≥7)forUCPH-102.AsmallbutsignificantdecreaseinthetotalexpressionlevelsofbothHA-EAAT1andHA-GLASTisobservedincellspreincubatedwith100μMUCPH-101(p=0.048)[1].PROTOCOLCellAssay[1]Cellsaresplitintopoly-D-lysine-coatedblack96-wellplateswithclearbottom.At16to24hlater,themediumisaspirated,andthecellsarewashedwith100μLKrebsbuffer[140mMNaCl/4.7mMKCl/2.5mMCaCl2/1.2mMMgCl2/11mMHEPES/10mMD-glucose,pH7.4];50μLKrebsbuffersupplementedwithvariousconcentrationsofUCPH-101orTBOAisaddedtothewells,afterwhichanadditional50μLKrebsbuffersupplementedwiththeFMPassaydye(1mg/mL)isaddedtoeachwell.Theplateisincubatedat37°Cinahumidified5%CO2incubatorfor30minandassayedinareadermeasuringemissionat560nmcausedbyexcitationat530nmbeforeandupto1minafteradditionof33μLGlusolution[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].AbrahamsenB,etal.Allostericmodulationofanexcitatoryaminoacidtransporter:thesubtype-selectiveinhibitorUCPH-101exertssustainedinhibitionofEAAT1throughanintramonomericsiteinthetrimerizationdomain.JNeurosci.2013Jan16;33(3):106McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.