UCPH-101-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEUCPH-101Cat.No.:HY-10914CASNo.:1118460-77-7分⼦式:C₂₇H₂₂N₂O₃分⼦量:422.48作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥50mg/mL(118.35mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3670mL11.8349mL23.6698mL5mM0.4734mL2.3670mL4.7340mL10mM0.2367mL1.1835mL2.3670mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.92mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性UCPH-101兴奋性氨酸转运⼦亚型1(EAAT1)的抑制剂，其IC50值为0.66μM。IC50&TargetIC50:0.66μM(EAAT1)[1]体外研究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.