LQVTDSGLYRCVIYHPP-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELQVTDSGLYRCVIYHPPCat.No.:HY-P3400CASNo.:887255-16-5分⼦式:C₈₉H₁₃₇N₂₃O₂₅S分⼦量:1961.25SequenceShortening:LQVTDSGLYRCVIYHPP作⽤靶点:Others作⽤通路:Others储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性LQVTDSGLYRCVIYHPP(LP17)⼀种髓系细胞表达的触发受体1(TREM-1)抑制肽。LQVTDSGLYRCVIYHPP显著减轻缺⾎诱导的梗死和神经元损伤。LQVTDSGLYRCVIYHPP可进⼊⼤脑，阻断TREM-1[1]。IC50&TargetTREM-1[1]体外研究LQVTDSGLYRCVIYHPP(LP17)(1or10ꢀμM;24h)substantiallydecreasesmRNAlevelsofpro-inflammatorycytokinesandchemokinesafterreoxygenationandremarkablyattenuatedextracellularproteinlevelsofIL-1βandIL-18inamicrogliaoxygen-glucosedeprivation(OGD)model[1].LQVTDSGLYRCVIYHPP(LP17)(10μM;24h)interactswithmicroglialSYK[1].RT-PCR[1]CellLine:PrimarymicrogliaConcentration:1or10ꢀμMIncubationTime:24hResult:DecreasedmRNAlevelsofNLRP3,IL-1β,IL-18,IL-6,CD16,CD32,iNOS,MCP-1,CXCL-1,andCXCL-2afterreoxygenation.WesternBlotAnalysis[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:PrimarymicrogliaConcentration:10ꢀμMIncubationTime:24hResult:Suppressedischemia/reperfusion-inducedincrementsinCARD9,p-p65inCARD9/NF-κBsignalingandNLRP3,ASC,cleavedcaspase-1,matureIL-1β,andmatureIL-18inNLRP3/caspase-1signalinginamicrogliaoxygen-glucosedeprivation(OGD)model.体内研究LQVTDSGLYRCVIYHPP(LP17)(0.5or1mg/kg;intranasal;dailyfor3days)alleviatesischemia-inducedinfarctionandneuronalinjuryinmice[1].AnimalModel:AdultmaleC57BL/6Jmice(20-25ꢀg),micecerebralischemia/reperfusion(I/R)modelinducedbymiddlecerebralarteryocclusion(MCAO)[1]Dosage:0.5ꢀmg/kgor1ꢀmg/kgAdministration:Intranasaladministration,oncedailyfor3consecutivedaysafterMCAOResult:Abolishedischemia-inducedTREM-1elevationat1ꢀmg/kg.Significantlyreducedinfarctvolumeby27.3%,inducedamarkedlyreductioninTUNELpositivecellsandFJCpositiveneuronsat1ꢀmg/kg.RescuedneurologicaldeficitsandcognitivedysfunctionofMCAOmice.InhibitedmicroglialM1polarizationandneutrophilinfiltration.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseo