Eltrombopag-SB-497115-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEltrombopagCat.No.:HY-15306CASNo.:496775-61-2Synonyms:SB-497115分⼦式:C₂₅H₂₂N₄O₄分⼦量:442.47作⽤靶点:ThrombopoietinReceptor;Bacterial;Apoptosis作⽤通路:Immunology/Inflammation;Anti-infection;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:8.33mg/mL(18.83mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2600mL11.3002mL22.6004mL5mM0.4520mL2.2600mL4.5201mL10mM0.2260mL1.1300mL2.2600mL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)1/5MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1mg/mL(2.26mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Eltrombopag(SB-497115)⼀种具有⼝服活性的thrombopoietin-receptor⾮肽激动剂。Eltrombopag可促⾎⼩板的活性，⽤于治疗⾎⼩板计数低的慢性免疫性⾎⼩板减少症。Eltrombopag可⽤于⼼⾎管的研究。Eltrombopag对多药耐药的⾦⾊葡萄球(Staphylococcusaureus)也有很强的抑制作⽤。Eltrombopag还可诱导肝癌细胞凋亡(apoptosis)。IC50&TargetThrombopoietinReceptor,Staphylococcusaureus,Apoptosis[1][3][5]体外研究Eltrombopag(0.002-50μM;4h)possessesactivityinmurineBAF3cellstransfectedwiththeluciferasereportergene[1].Eltrombopag(30μM;120min)affectstheactivatesofp-STAT5inN2C-Tpocells[1].Eltrombopag(30μM;120min)activatesp-STAT5inmegakaryocytes[1].Eltrombopag(0.1nM-10μM;30min)stimulatesproliferationofBAF3/hTpoRcells[1].Eltrombopag(0.03-3μM;10days)increasesthedifferentiationofbonemarrowCD34+cellsintoCD41+megakaryocytes[1].Eltrombopag(0-3μM;72h)affectsN2C-Tpocellapoptosis[1].EltrombopagefficientlyinhibitsPneumococcalgrowthwithMIC50of0.3mg/L,butshowsnoactivityagainstGram-negativebacteria[3].Eltrombopag(0-200mg/L;24h;Caco-2andHepG2cells)inhibitsStaphylococcusaureusgrowthwithanMIC50of1.5mg/L,andexhibitshigherpotencywhenco-treatswithVancomycin(HY-B0671)withanMIC50of1.2mg/L[3].Eltrombopag(0or10μg/mL;72h)significantlyinducesG0/G1phasearrestinHuh7cells[5].Eltrombopag(0.1-100μg/mL;72h)exhibitsanti-proliferativeactivityagainstHCCcelllines[5].CellViabilityAssay[1]CellLine:MurineBAF3cellsConcentration:0.002-50μMIncubationTime:4hResult:EffectivelyinhibitedmurineBAF3cellswithhumanTpoRwithanEC50valueof0.27μM.[1][1]CellLine:N2C-TpocellsandCD34+Concentration:30μMforN2C-Tpocells;0,1,3and10μMforCD34+IncubationTime:120minforN2C-Tpocells;30minforCD34+Result:Activatedphospho-STAT5andmaximumsignalintensityexhibitedat60minutesaftertreatmentinN2C-Tpocells.2/5MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDose-dependentlyactivatedSTAT5phosphorylationat30minutesaftertreatmentinCD34+.CellProliferationAssay[1]CellLine:BAF3/hTpoRcellsConcentration:0.1nM-10μMIncubationTime:2daysResult:PromotedBAF3/hTpoRcellsproliferationafterincubatedfor2dayswithanEC50of0.03μM.CellDifferentiationAssay[1]CellLine:CD34+Concentration:0.003,0.01,0.03,0.1,0.3,1and3μMIncubationTime:10daysResult:Dose-dependentlystimulatedthedifferentiationfrombonemarrowCD34+cellstoCD41+megakaryocyteswithanEC50valueof0.1μM.ApoptosisAnalysis[1]CellLine:N2C-TpocellsConcentration:0,0.003,0.01,0.03,0.1,0.3,1and3μMIncubationTime:72hoursResult:Exhibiteddose-dependentlyantiapoptoticeffectsN2C-Tpocellswithaconcentrationover0.03μM.CellProliferationAssay[5]CellLine:Huh7,HepG2andHep3Bcells(preloadedwithiron(500μg/mlFAC)for24h)Concentration:0.1-100μg/mLIncubationTime:72hResult:Exhibitedanti-proliferativeactivityagainstHCCcelllineswithIC50sof5.7μg/mlforHuh7,5.4μg/mlforHepG2,and4.7μg/mlforHep3B.CellCycleAnalysis[5]3/5MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:Huh7cellsConcentration:0or10μg/mLIncubationTime:72hResult:SignificantlyinducedG0/G1phasearrest.体内研究EltrombopagOlamine(10mg/kg;p.o.onceadayfor5days)showsgoodtoleranceinchimpanzees[1].EltrombopagOlamine(17.6mg/kg;i.p.;onceadayfor2days)significantlyreducesmeanS.aureuscountsinmicenasalinfection[3].AnimalModel:Femalechimpanzees[1]Dosage:10mg/kgAdministration:Oralgavage;10mg/kgonceaday;for5daysResult:Appearedagoesupandthengoesbacktendencyofplateletcountsaftertreatment,andshowednobadeffectsofhematology,coagulation,orclinicalchemistryparametersonanimal.AnimalModel:C57BL/6malemice(7weeks,20-22g;injectedS.aureus(5×108CFUsuspendedin40µLPBS)intothenasalcavities)[3]Dosage:17.6mg/kgAdministration:IP;onceadayfor2daysResult:Significantlyreducedmeanbacterialcounts(5.0×106CFU/lung)inthenasalinfectionmodelcomparedwithcontrolPBS(5.2×107CFU/lung)mice.户使⽤本产品发表的科研⽂献•Cells.2022,11(3),319.•BloodAdv.2017Feb28;1(7):468-476.•FrontPharmacol.2020Nov16;11:582625.•JThrombHaemost.2022May27.•Viruses.2019Apr25;11(4):385.Seemorecustomervalidationsonwww.MedChemEREFERENCES4/5MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].Erickson-MillerCL,etal.Discoveryandcharacterizationofaselective,nonpeptidylthrombopoietinreceptoragonist.ExpHematol.2005Jan;33(1):85-93.[2].LeeH,etal.RepurposingEltrombopagforMultidrugResistantStaphylococcusaureusInfections.Antibiotics(Basel).2021Nov9;10(11):1372.[3].JuanZhu,et