EG01377-dihydrochloride-DataSheet-生命科學(xué)試劑-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEEG01377dihydrochlorideCat.No.:HY-112151A分?式:C??H??Cl?N?O?S?分?量:659.6作?靶點:ComplementSystem作?通路:Immunology/Inflammation儲存?式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實驗DMSO:200mg/mL(303.21mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5161mL7.5804mL15.1607mL5mM0.3032mL1.5161mL3.0321mL10mM0.1516mL0.7580mL1.5161mL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，并請注意儲備液的保存?式和期限。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，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；澄的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(7.58mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(7.58mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(7.58mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE?物活性EG01377dihydrochloride有效的、可?物利?的和選擇性的neuropilin-1(NRP1)抑制劑，Kd值為1.32μM，對NRP1-a1和NRP1-b1的IC50值均為609nM。EG01377dihydrochloride具有抗?管?成，抗遷移及抗腫瘤等活性。IC50&TargetIC50:609nM(NRP1-a1andNRP1-b)[1]體外研究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.體內(nèi)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?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedforme