C29-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEC29Cat.No.:HY-100461CASNo.:363600-92-4分⼦式:C₁₆H₁₅NO₄分⼦量:285.29作⽤靶点:Toll-likeReceptor(TLR)作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥30mg/mL(105.16mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.5052mL17.5260mL35.0521mL5mM0.7010mL3.5052mL7.0104mL10mM0.3505mL1.7526mL3.5052mL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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(8.76mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.76mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性C29⼀种Toll-likereceptor2(TLR2)抑制剂。C29阻断hTLR2/1和hTLR2/6信号，IC50值分别为19.7和37.6μM。IC50&TargetTLR2体外研究C29(10or50μΜ;1hour)blocksP3C-andP2C-inducedIL-8mRNAdose-dependentlyinHEK-TLR2stabletransfectants.C29(50-200μM;1hour)inhibitsP3C-andP2C-inducedIL-1βgeneexpressionsignificantlyatboth1hand4hfollowingstimulationinTHP-1cells[1].C29(25or50μΜ;1hour)reducesP3C-inducedbutnotP2C-inducedTNF-αmRNAandIL-12p40proteinsignificantlyinprimarymurinemacrophages[1].C29(50μΜ;1hour)blocksTLR2bacterialagonist-inducedproinflammatorygeneexpressioninHEK-TLR2cellsandmurinemacrophages[1].WesternBlotAnalysis[1]CellLine:THP-1cellsConcentration:150μMIncubationTime:1hoursResult:DiminishedtheinteractionbetweenendogenousTLR2andmyeloiddifferentiationprimaryresponsegene88(MyD88)at15and30minpoststimulationwithP3C.WesternBlotAnalysis[1]CellLine:MurineperitonealmacrophagesConcentration:50μMIncubationTime:1hoursResult:BlockedrobustMAPKactivationat30minandreducedNF-κBactivationfrom5to30min.PreventedP3C-induceddegradationofIκBαat15and30min.户使⽤本产品发表的科研⽂献•NatImmunol.2021Jul;22(7):829-838.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•Biomaterials.2020May;241:119852.•JControlRelease.2020Dec10;328:210-221.•BMCMed.2021Oct15;19(1):247.•CarbohydrPolym.15September2022,119683.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CaiS,ZhuG,CenX,etal.Synthesis,structure-activityrelationshipsandpreliminarymechanismstudyofN-benzylideneanilinederivativesaspotentialTLR2inhibitors.BioorgMedChem.2018;26(8):2041-2050.[2].MistryP,etal.InhibitionofTLR2signalingbysmallmoleculeinhibitorstargetingapocketwithintheTLR2TIRdomain.ProcNatlAcadSciUSA.2015Apr28;112(17):5455-60.McePdfHeightCaution:Producthasnotbeenfullyvalidated