BIA-10-2474-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBIA10-2474Cat.No.:HY-19740CASNo.:1233855-46-3分?式:C??H??N?O?分?量:300.36作?靶點:FAAH;Autophagy作?通路:MetabolicEnzyme/Protease;NeuronalSignaling;Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:2.2mg/mL(7.32mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.3293mL16.6467mL33.2934mL5mM0.6659mL3.3293mL6.6587mL10mM---------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。-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BIA10-2474脂酸酰胺?解酶FAAH的抑制劑，對???腦不同區(qū)域的IC50值為50?70mg/kg。IC50&TargetIC50:50-70mg/kg(FAAH,ratbrainregions)[1]體外研究ExVivo:BIA10-2474provestobeapotentFAAHinhibitorwithIC50sof50-70mg/kg(i.p.)invariousbrain1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEregions.IC50valuesforbrainregionsare52(cerebellum),67(restofbrain),68(cortex),and71mg/kg(hypothalamus)[1].體內(nèi)研究InJanuary2016,severeadverseevents(SAE)occursinthePhaseIclinicaltrialusingthedrugBIA10-2474includingonedeath.Thepossibilitiesforfailureoftrialssuchasoff-targeteffect,dosecalculation,unexpectedimmuneresponse,speciesvariation,andcumulativedosetoxicitywouldbesought[2].PROTOCOLAnimalRats:Groupsofrats(n=4)arepre-treatedwithBIA10-2474(2mL/kgin5%Tween80insalinei.p.)orwithAdministration[1]vehicle40minpriortoradiotracerinjection.Rats,inarestrainingbox,receives3–4MBqofhigh-specificactivity[18F]-DOPPin0.3mLof10%ethanolincitratebuffer(pH6)viathetailveinwhichhasbeenvasodilatedinawarmwaterbath.Theyaresacrificedbydecapitationat40minafterradiotraceradministration,thebrainissurgicallyremovedfromtheskullandstoredonice.Brainregionsareexcised,blotted,andweighedwhilebloodiscollected.Radioactivityintissuesisassayed[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻?CellDeathDiffer.2022Sep14.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TongJ,etal.InhibitionoffattyacidamidehydrolasebyBIA10-2474inratbrain.JCerebBloodFlowMetab.2016Sep20.[2].KaurR,etal.WhatfailedBIA10-2474PhaseIclinicaltrial?GlobalspeculationsandrecommendationsforfuturePhaseItrials.JPharmacolPharmacother.2016Jul-Sep;7(3):120-6McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.