M1001-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEM1001Cat.No.:HY-111547CASNo.:874590-32-6分⼦式:C₁₇H₁₇N₃O₂S分⼦量:327.4作⽤靶点:HIF/HIFProlyl-Hydroxylase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(763.59mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0544mL15.2718mL30.5437mL5mM0.6109mL3.0544mL6.1087mL10mM0.3054mL1.5272mL3.0544mL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%salineSolubility:≥2.33mg/mL(7.12mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性M1001⼀种较弱的低氧诱导因⼦-2α(HIF-2α)激动剂。M1001可以与HIF-2αPAS-B结构域结合，其Kd值为667nM。M1001可⽤于慢性肾脏病的研究。IC50&TargetKd:667nM(HIF-2α)[1]体外研究M1001(10ꢀµM)treatmentshowsincreasedexpressionofHIF-2targetgenesin786-Ocells[1].M1001(10ꢀµM)bindstoHIF-2αandhasthepropertiesofaweakagonist[1].M1001(1-10ꢀµM)reducesVHLbindingtoHIF-2α[1].WesternBlotAnalysis[1]CellLine:786-OcellsConcentration:10ꢀµMIncubationTime:Result:IncreasedtheexpressionofHIF-2targetgenesmodestlyin786-Ocells.WesternBlotAnalysis[1]CellLine:HEK293TcellsConcentration:1and10ꢀµMIncubationTime:Result:ReducedthephysicalassociationbetweenHIF-2αandVHL.REFERENCES[1].WuD,etal.BidirectionalmodulationofHIF-2activitythroughchemicalligands.NatChemBiol.2019Feb25.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-37