Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESPHINXCat.No.:HY-132126CASNo.:848057-98-7分?式:C??H??F?N?O?分?量:354.32作?靶點(diǎn):SRPK作?通路:CellCycle/DNADamage儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(141.12mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.8223mL14.1115mL28.2231mL5mM0.5645mL2.8223mL5.6446mL10mM0.2822mL1.4112mL2.8223mLBIOLOGICALACTIVITY?物活性SPHINXSRPK1的選擇性抑制劑，IC50值為0.58μM。SPHINX有效地減少體內(nèi)脈絡(luò)膜新??管(CNV)。SPHINX可?于?年性斑變性的研究。IC50&TargetIC50:0.58μM(SRPK1)[1]體外研究SPHINX(10μM;2h)affectsEGF-inducedphosphorylationofSRSF1andSRSF2[1].SPHINX(5μM;24h)reducestheexpressionofVEGF165relativetoGAPDHcontroleitherinprimaryRPEandARPE-19celllines[1].WesternBlotAnalysis[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:ARPE-19celllineConcentration:10μMIncubationTime:2hoursResult:BlockedEGF-inducedphosphorylationofSRSF1andSRSF2.體內(nèi)研究SPHINX(10ng;i.o.onlaserphotocoagulationday0andday7)affectsneovasculargrowthinvivo[1].SPHINX(25ng;i.o.onlaserphotocoagulationday0andday7)affectstheCNVareainCNVrats[1].AnimalModel:C57/B6micewithlaser-inducedCNV[1]Dosage:10ngAdministration:Intraocularinjection;10ngonlaserphotocoagulationday0andday7Result:Significantlyreducedneovasculargrowthcomparedwithsaline-injectedcontrols.AnimalModel:NorwayBrownratswithlaser-inducedchoroidalneovascularization[1]Dosage:25ng(10ng/uL)Administration:Intraocularinjection;25ng(10ng/uL)onlaserphotocoagulationday0andday7Result:SignificantlyreducedtheCNVareacomparedwithsalineinjectedcontrols.REFERENCES[1].GammonsMV,etal.TopicalantiangiogenicSRPK1inhibitorsreducechoroidalneovascularizationinrodentmodelsofexudativeAMD.InvestOphthalmolVisSci.2013Sep5;54(9):6052-62.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: