CYB210010-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECYB210010Cat.No.:HY-162423CASNo.:2762568-47-6分⼦式:C₁₁H₁₅ClF₃NO₂S分⼦量:317.76作⽤靶点:5-HTReceptor;AndrogenReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling;VitaminDRelated/NuclearReceptor储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性CYB210010具有⼝服⽣物利⽤度且长效的⾎素5-HT2受体激动剂，可选择性靶向5-HT2A和5-HT2C受体(EC50:4.1nM和7.3nM)。CYB210010可进⼊中枢神经系统，引起头部抽搐反应(HTR)，且不容易在慢性给药过程中出现⾏为耐受性。IC50&Target5-HT1AReceptor5-HT1BReceptor5-HT6Receptor5-HT7Receptor32nM(Ki)949nM(Ki)1301nM(Ki)4918nM(Ki)5-HT2AReceptor5-HT2CReceptor5-HT2BReceptor4.1nM(EC50)7.3nM(EC50)88nM(EC50)体内研究CYB210010hascertainoralbioavailabilityandcansmoothlyenterthecentralnervoussystem,bindto5-HT2Areceptorsinthefrontalcortex,andincreasetheexpressionofneuroplasticity-relatedgenesinthefrontalcortex[1].CYB210010(0.1-3mg/kg;sc;singledose)causesaheadtwitchresponse(HTR)inmouse,andcanbeadministeredsubchronicallyatthresholddoseswithoutdevelopingbehavioraltolerance[1].AnimalModel:MaleC57BL/6Jmice[1]Dosage:0.1,0.3,1,3,mg/kgAdministration:sc;sigledoseResult:ElicitedmaximumHTRsat-15minpostadministrationwhichterminatedafter220min1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE(significantfromvehiclefrom5-160min).REFERENCES[1].VartyGB,etal.SynthesisandStructure-ActivityRelationshipsof2,5-Dimethoxy-4-SubstitutedPhenethylaminesandtheDiscoveryofCYB210010:APotent,OrallyBioavailableandLong-ActingSerotonin5-HT2ReceptorAgonist.JMedChem.2024Apr25;67(8):6144-6188.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;0