LY-450139isaγ-secretaseinhibitorthatsuppressesNotchsignalingandexhibitsneuroprotectiveactivity.LY-450139displaysmixedresultsinclinicaltrialsasapotentialtreatmentforAlzheimer’sdisease.ThiscompoundalsoincreasesglutamateintheprefrontalcortexwhenadmiNISTeredchronicallyandactivatesgrowthhormonesecretagoguereceptorGHS-R1a.
| CasNo. | 425386-60-3 |
|---|---|
| Purity | ≥98% |
| Formula | C19H27N3O4 |
| FormulaWt. | 361.44 |
| IUPACName | (2S)-2-Hydroxy-3-methyl-N-[(2S)-1-{[(1S)-3-methyl-2-oxo-2,3,4,5-tetrahydro-1H-3-benzazepin-1-yl]amino}-1-oxo-2-propanyl]butanamide |
| Synonym | Semagacestat |
| Appearance | Whitetooffwhitepowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | L9701InfoSheetPDF |
|---|
BeggiatoS,GiulianiA,SiviliaS,etal.CHF5074andLY450139sub-acutetreatmentsdifferentlyaffectcorticalextracellularglutamatelevelsinpre-plaqueTg2576mice.Neuroscience.2014Apr25;266:13-22.PMID:24530449.
DoodyRS,RamanR,FarlowM,etal.Aphase3trialofsemagacestatfortreatmentofAlzheimer"sdisease.NEnglJMed.2013Jul25;369(4):341-50.PMID:23883379.
SchellekensH,McNamaraO,DinanTG,etal.Semagacestat,aγ-secretaseinhibitor,activatesthegrowthhormonesecretagogue(GHS-R1a)receptor.JPharmPharmacol.2013Apr;65(4):528-38.PMID:23488781.
