Eltrombopag-SB-497115-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEltrombopagCat.No.:HY-15306CASNo.:496775-61-2Synonyms:SB-497115分?式:C??H??N?O?分?量:442.47作?靶點:ThrombopoietinReceptor;Bacterial;Apoptosis作?通路:Immunology/Inflammation;Anti-infection;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:8.33mg/mL(18.83mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2600mL11.3002mL22.6004mL5mM0.4520mL2.2600mL4.5201mL10mM0.2260mL1.1300mL2.2600mL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；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1/5MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1mg/mL(2.26mM);ClearsolutionBIOLOGICALACTIVITY?物活性Eltrombopag(SB-497115)?種具有?服活性的thrombopoietin-receptor?肽激動劑。Eltrombopag可促??板的活性，?于治療??板計數(shù)低的慢性免疫性??板減少癥。Eltrombopag可?于??管的研究。Eltrombopag對多藥耐藥的??葡萄球(Staphylococcusaureus)也有很強(qiáng)的抑制作?。Eltrombopag還可誘導(dǎo)肝癌細(xì)胞凋亡(apoptosis)。IC50&TargetThrombopoietinReceptor,Staphylococcusaureus,Apoptosis[1][3][5]體外研究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?邊的抑制劑?師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?邊的抑制劑?師www.MedChemECellLine:Huh7cellsConcentration:0or10μg/mLIncubationTime:72hResult:SignificantlyinducedG0/G1phasearrest.體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師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