Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBNS808Cat.No.:HY-172808CASNo.:2836313-12-1分?式:C??H??Cl?N?O?S分?量:548.87作?靶點:CannabinoidReceptor;CytochromeP450作?通路:GPCR/GProtein;NeuronalSignaling;MetabolicEnzyme/Protease儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性BNS808?種有?服活性的選擇性CB1R拮抗劑(IC50=0.8nM)，并具有顯著的CB2R選擇性和極低的腦滲透性。BNS808正?于研究肥胖及其相關的代謝并發(fā)癥，例如代謝功能障礙相關的脂肝(MASLD)。BNS808降低了藥物進?中樞神經系統(tǒng)的游離利?率，從?提?了安全性，并通過??漿結合率最?限度地減少了藥物間相互作?[1]。IC50&TargetCYP2C9CYP2C19CYP1A2CYP2D62.99μM(IC50)8.33μM(IC50)18.0μM(IC50)>50μM(IC50)CB1R0.8nM(IC50)體外研究BNS808(72h)displaysverylowcytotoxicityinHepG2cellswithanIC50of16.84μM[1].BNS808demonstratesahERGIC50of5.39μMsuggestinglowpotentialforcardiotoxicitysinceitsIC50forCB1Ris0.8nM[1].BNS808(0.2mg/mL,10min)exhibitsmoderateinhibitionofCYP3A4,weak-moderateinhibitionofCYP2C9andCYP2C19,andweakinhibitionofCYP1A2andCYP2D6,withIC50valuesof2.99,8.33,18.0,and>50μM,respectively[1].體內研究BNS808(1mg/kg,p.o.,onesingledose)demonstrateslimitedbrainpenetrance(anaverageof13.7ng/g)afterasingledoseatdifferenttimepoints(1-8h)inC57Bl/6mice[1].BNS808(1mg/kg,p.o.,24d)demonstrateslimitedbrainpenetrance(around20ng/g)afterchronicadministrationinC57Bl/6mice[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBNS808(1-10mg/kg,p.o.)showsnoCNS-mediatedsideeffectsinwide-typemaleC57Bl/6Jmiceatlow(1mg/kg)andhigh(10mg/kg)dosesandnosignificantchangesinlocomotoractivity[1].BNS808(1mg/kg/day,p.o.,24days)reducesbodyweightandimprovesmetabolicprofileindiet-inducedobese(DIO)C57Bl/6Jmice[1].AnimalModel:Diet-inducedobese(DIO)maleC57Bl/6Jmice[1]Dosage:1mg/kg/day,24daysAdministration:Oralgavage(p.o.)Result:Reducedbodyweightattributingtoareductionintotalbodyfatwithasignificantincreaseinleanbodymass.Suggestedatrendtowardsubstantialeffectsofthedrugonglucosehomeostasisandreducedglucoselevelsinfastingconditions.Demonstratedefficacyinreversinghepaticsteatosisandhepatocellulardamage.Ledtoasignificantreductioninlivertriglyceridecontentandliverenzymes,includingALT,AST,andALP.REFERENCES[1].GammalA,etal.,SynthesisandPharmacologicalCharacterizationofNovelPeripheralCannabinoid-1ReceptorBlockersBasedonaTricyclicScaffold.JMedChem.2025Apr21.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.