EG01377-dihydrochloride-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEEG01377dihydrochlorideCat.No.:HY-112151A分⼦式:C₂₆H₃₂Cl₂N₆O₆S₂分⼦量:659.6作⽤靶点:ComplementSystem作⽤通路:Immunology/Inflammation储存⽅式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:200mg/mL(303.21mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5161mL7.5804mL15.1607mL5mM0.3032mL1.5161mL3.0321mL10mM0.1516mL0.7580mL1.5161mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(7.58mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(7.58mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(7.58mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性EG01377dihydrochloride有效的、可⽣物利⽤的和选择性的neuropilin-1(NRP1)抑制剂，Kd值为1.32μM，对NRP1-a1和NRP1-b1的IC50值均为609nM。EG01377dihydrochloride具有抗⾎管⽣成，抗迁移及抗肿瘤等活性。IC50&TargetIC50:609nM(NRP1-a1andNRP1-b)[1]体外研究EG01377(3-30μM;30minutes)inhibitsvascularendothelialgrowthfactorA(VEGF-A)stimulatedtyrosinephosphorylationofVEGF-R2/KDR[1].EG01377(30μM)isabletosignificantlyreduceHUVECcellmigrationinresponsetoVEGFA[1].EG01377(30μM;5days)candelaytheVEGF-inducedwoundclosure[1].EG01377(30μM)reducesnetworkarea,length,andbranchingpoints[1].EG01377(30μM;7days)reducesVEGF-inducedangiogenesis[1].EG01377(30μM;7days)incombinationwithVEGFAreducesA375P(malignantmelanoma)spheroidoutgrowth[1].EG01377(500nM;2hours)blockstheproductionoftransforminggrowthfactorbeta(TGFβ)byNrp1+regulatoryT-cellSMAD3/AKT(Tregs)inthepresenceoftumorcell-derivedfactors[1].WesternBlotAnalysis[1]CellLine:Humanumbilicalveinendothelialcells(HUVECs)Concentration:3,10,30μMIncubationTime:30minutesResult:InhibitedVEGF-AstimulatedtyrosinephosphorylationofVEGF-R2/KDRwithanIC50of30μM.体内研究EG01377(2mg/kg;i.v.)exhibitsanencouraginghalf-lifeof4.29h,sufficienttosustainonceperdaydosinginmice[1].AnimalModel:6-8week-oldBABL/cfemalemice[1]Dosage:2mg/kg(PharmacokineticAnalysis)Administration:I.v.administrationResult:Thehalftime(T1/2)of4.29h.REFERENCES[1].PowellJ,etal.SmallMoleculeNeuropilin-1AntagonistsCombineAntiangiogenicandAntitumorActivitywithImmuneModulationthroughReductionofTransformingGrowthFactorBeta(TGFβ)ProductioninRegulatoryT-Cells.JMedChem.2018May10;61(9):4135-4154.McePdfHeight2/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedforme