Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEBChE-IN-44Cat.No.:HY-178356分子式:C??H??N?O?分子量:393.44作用靶點:Cholinesterase(ChE);nAChR;InterleukinRelated;TNFReceptor作用通路:NeuronalSignaling;MembraneTransporter/IonChannel;Immunology/Inflammation;Apoptosis儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性 BChE-IN-44是一種高效、可穿透血腦屏障、高選擇性的丁酰膽堿酯酶(BChE)抑制劑[equineBChEIC50=18.00pM，humanBChEIC50=1.50nM]。BChE-IN-44對Aβ1-42誘導(dǎo)的損傷模型具有神經(jīng)保護作用，并能抑制Aβ1-42的自聚集。BChE-IN-44可降低Lipopolysaccharides(HY-D1056)誘導(dǎo)的BV2細胞中炎癥因子(NO、IL-6和TNF-α)的水平。BChE-IN-44可顯著改善Scopolamine(HY-N0296)誘導(dǎo)的認知障礙。BChE-IN-44能夠調(diào)節(jié)小鼠海馬體中BChE和acetylcholine的水平。BChE-IN-44可用于阿爾茨海默病(AD)的研究[1]。IC50&TargetIL-6RatBuChE體外研究BChE-IN-44(CompoundN14)(50μM,24h)leadtoabout15%celltoxicityinPC12andSH-SY5Y,suggestingthatBChE-IN-44possessesahighsafetyprofileinvitro[1].BChE-IN-44showsaKcof0.017μM,indicatingthatBChE-IN-44possessesahigheraffinityforBChE[1].BChE-IN-44(5-20μM,24h)significantlyreducesthelevelsofinflammatoryfactors(NO,IL-6,andTNF-α)inLipopolysaccharides(LPS)-inducedBV2cells[1].BChE-IN-44(20μM,24h)demonstratessignificantneuroprotectiveefficacyagainstAβ1–42-inducedinjuryinPC12cells[1].BChE-IN-44(20μM,48h)effectivelyinhibitsAβ1-42aggregation,confirmingthegoodinhibitoryeffectsofthecarrierscaffoldonAβ1–42aggregation[1].CellViabilityAssay[1]CellLine:PC12cells,SH-SY5YcellsConcentration:50μM1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEIncubationTime:24hResult:Ledtoabout15%celltoxicityinPC12andSH-SY5Y.ELISAAssay[1]CellLine:BV2cellsConcentration:5μM,10μM,20μMIncubationTime:24hResult:Significantlyreducedthelevelsofinflammatoryfactors(NO,IL-6,andTNF-α)inLPS-inducedBV2cells.CellViabilityAssay[1]CellLine:PC12cellsConcentration:20nMIncubationTime:24hResult:ShowedsignificantneuroprotectiveefficacyagainstAβ1-42-inducedinjuryinPC12cells.體內(nèi)研究BChE-IN-44(5-20mg/kg,i.p.,oncedailyfor14days)caneffectivelyreverseScopolamine-inducedcognitiveimpairment,anxiety,andlearningandmemorydeficitsinmice,inhibitBChEactivity,increaseAChlevels,andreduceneuroinflammation[1].AnimalModel:Thirty-sixsix-week-oldmaleKunmingmice(weighing25-30g)wereintraperitoneallyinjectedwithscopolamine(3mg/kg)tomimicAD-likecognitivedeficits[1].Dosage:5mg/kg,10mg/kg,20mg/kgAdministration:I.p.,oncedailyfor14days,30minsafterScopolamineResult:Increasedthespontaneousalternationrateto72.6%,indicatingimprovedworkingmemory.Increasedcentralregiondwelltimeandtraveldistance,andreducedanxiety-likebehaviors.Shortenedescapelatency,reducedtraveldistance,andincreasedplatformcrossings,showingimprovedspatiallearningmemory.Behavioraltrajectoryplotsshowedmoreorganized.IncreasesAChlevelsanddecreasesAChEandBChEactivities.ReducesIL-6andTNF-αlevelsandinhibitsneuroinflammation.2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEREFERENCESZhaoY,etal.DiscoveryofahighlyselectiveBChEinhibitorwithconcomitantanti-neuroinflammatoryactivityfortreatingAlzheimer'sdisease.EurJMedChem.2025Dec5;299:118071.McePdfHeightCaution:Producthasnotbeenf