M62812-DataSheet-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEM62812Cat.No.:HY-103639ACASNo.:613263-00-6分?式:C??H??Cl?N?OS分?量:330.23作?靶點:Toll-likeReceptor(TLR)作?通路:Immunology/Inflammation儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗H2O:10mg/mL(30.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.0282mL15.1410mL30.2819mL5mM0.6056mL3.0282mL6.0564mL10mM0.3028mL1.5141mL3.0282mL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(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性M62812?種toll樣受體4(TLR4)信號轉(zhuǎn)導抑制劑。M62812可抑制內(nèi)?細胞和?細胞活化，防???發(fā)?致死性感染性休克。M62812可以降低LPS誘導的凝?反應和炎癥反應。M62812可?于膿毒癥的研究[1]。體外研究M62812(10μg/mL;6h)completelyinhibitsLPS-inducedNF-κBactivationinNF-κBluciferase-expressingcellswithanIC50of2.4μg/mL[1].M62812(3μg/mL;6h)completelyinhibitsLPS-inducedTNF-αproductioninperipheralbloodmononuclear1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEcellswithanIC50of0.7μg/mL[1].M62812(3μg/mL;6h)completelyinhibitstheproductionofIL-6andE-selectioninhumanendothelialcellswithIC50sof0.43μg/mLand1.4μg/mL[1].體內(nèi)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