M1001-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEM1001Cat.No.:HY-111547CASNo.:874590-32-6分?式:C??H??N?O?S分?量:327.4作?靶點:HIF/HIFProlyl-Hydroxylase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(763.59mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.0544mL15.2718mL30.5437mL5mM0.6109mL3.0544mL6.1087mL10mM0.3054mL1.5272mL3.0544mL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%salineSolubility:≥2.33mg/mL(7.12mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性M1001?種較弱的低氧誘導因?-2α(HIF-2α)激動劑。M1001可以與HIF-2αPAS-B結(jié)構(gòu)域結(jié)合，其Kd值為667nM。M1001可?于慢性腎臟病的研究。IC50&TargetKd:667nM(HIF-2α)[1]體外研究M1001(10?μM)treatmentshowsincreasedexpressionofHIF-2targetgenesin786-Ocells[1].M1001(10?μM)bindstoHIF-2αandhasthepropertiesofaweakagonist[1].M1001(1-10?μM)reducesVHLbindingtoHIF-2α[1].WesternBlotAnalysis[1]CellLine:786-OcellsConcentration:10?μMIncubationTime:Result:IncreasedtheexpressionofHIF-2targetgenesmodestlyin786-Ocells.WesternBlotAnalysis[1]CellLine:HEK293TcellsConcentration:1and10?μMIncubationTime:Result:ReducedthephysicalassociationbetweenHIF-2αandVHL.REFERENCES[1].WuD,etal.BidirectionalmodulationofHIF-2activitythroughchemicalligands.NatChemBiol.2019Feb25.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-37