nAChR-antagonist-2-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEnAChRantagonist2Cat.No.:HY-180559分⼦式:C₂₃H₃₂INO₂分⼦量:481.41作⽤靶点:nAChR;InterleukinRelated作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling;Immunology/Inflammation储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性nAChRantagonist2⼀种选择性nAChR拮抗剂。nAChRantagonist2在⾮洲⽖蟾母细胞中对包括⼈源α9α10、α9和α7在内的nAChR亚型表现出抑制活性，其IC50值分别为16.0nM、26.2nM和336.3nM。nAChRantagonist2能在纳尔浓度⽔平抑制ATP诱导的IL-1β释放。nAChRantagonist2可⽤于⾮阿⽚类镇痛药和免疫调节剂的相关研究[1]。IC50&TargetIL-1β体外研究nAChRantagonist2(compound22)(300pM-30μM,3min)selectivelyinhibitsACh-evokedcurrentsmediatedbyα9-containingnAChRsexpressedinXenopusoocytes,withIC50valuesof16.0nM,26.2nM,and336.3nMforhα9α10,hα9,andhα7,respectively[1].nAChRantagonist2(100pMor100nM,40min)exertsbothantagonisticandagonisticfunctionsattheNCNRsofmonocyticTHP-1cells[1].ELISAAssay[1]CellLine:THP-1cellswereprimedwithLipopolysaccharide(HY-D1056)(1μg/mL,5h),followedby40minofBzATPtriethylammoniumsalt(HY-136254)(40min)[1]Concentration:100pMor100nMIncubationTime:40minResult:EfficientlyantagonizedtheinhibitoryeffectofAchat100pM.Exhibtedmildantagonisticeffectsathigher100nM.EffectivelyandsignificantlyinhibitedtheBzATP(HY-136254)-inducedreleaseofIL-1βin1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEtheabsenceofACh.REFERENCES[1].GiraudoA,etal.DualAgonist/AntagonistModulationofα9-ContainingNicotinicAcetylcholineReceptorsby2-AmmoniumethylEthersofStilbenolandStilbenolAnalogues.JMedChem.2025Dec25;68(24):26099-26120.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;