M62812-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEM62812Cat.No.:HY-103639ACASNo.:613263-00-6分⼦式:C₁₃H₁₃Cl₂N₃OS分⼦量:330.23作⽤靶点:Toll-likeReceptor(TLR)作⽤通路:Immunology/Inflammation储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验H2O:10mg/mL(30.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0282mL15.1410mL30.2819mL5mM0.6056mL3.0282mL6.0564mL10mM0.3028mL1.5141mL3.0282mL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(sealedstorage,awayfrommoisture)。-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。BIOLOGICALACTIVITY⽣物活性M62812⼀种toll样受体4(TLR4)信号转导抑制剂。M62812可抑制内⽪细胞和⽩细胞活化，防⽌⼩⿏发⽣致死性感染性休克。M62812可以降低LPS诱导的凝⾎反应和炎症反应。M62812可⽤于脓毒症的研究[1]。体外研究M62812(10μg/mL;6h)completelyinhibitsLPS-inducedNF-κBactivationinNF-κBluciferase-expressingcellswithanIC50of2.4μg/mL[1].M62812(3μg/mL;6h)completelyinhibitsLPS-inducedTNF-αproductioninperipheralbloodmononuclear1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEcellswithanIC50of0.7μg/mL[1].M62812(3μg/mL;6h)completelyinhibitstheproductionofIL-6andE-selectioninhumanendothelialcellswithIC50sof0.43μg/mLand1.4μg/mL[1].体内研究M62812(i.v.;10-20mg/kg;singledose)isprotectiveandreducesinflammatoryandcoagulationparametersinaD-galactosamine-sensitizedendotoxinshockmousemodel[1].M62812(i.v.;20mg/kg;onceadayforthreedays)preventsmicefromlethalityinamurinececalligationandpuncturemodel[1].AnimalModel:D-galactosamine-sensitizedendotoxinshockmousemodel[1]Dosage:10-20mg/kgAdministration:Intravenousadministration(i.v.)Result:PreventedelevationofTNF-α,IL-6,solubleE-selectin,thrombin/antithrombincomplexesandglutamicpyruvictransaminaseactivityat20mg/kg.Prolongedsurvivalinad-galactosamine-sensitizedendotoxinshockmousemodel.AnimalModel:Cecalligationandpuncturemousemodel[1]Dosage:20mg/kgAdministration:Intravenousadministration(i.v.);onceadayforthreedaysResult:Reducedmortalityinamurinececalligationandpuncturemodel.REFERENCES[1].NakamuraM,etal.Toll-likereceptor4signaltransductioninhibitor,M62812,suppressesendothelialcellandleukocyteactivationandpreventslethalsepticshockinmice.EurJPharmacol.2007Aug27;569(3):237-43.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For