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LY-450139 is a γ-secretase inhibitor that suppresses Notch signaling and exhibits neuroprotective activity. LY-450139 displays mixed results in clinical trials as a potential treatment for Alzheimer’s disease. This compound also increases glutamate in the prefrontal cortex when administered chronically and activates growth hormone secretagogue receptor GHS-R1a.
| Cas No. | 425386-60-3 |
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| Purity | ≥98% |
| Formula | C19H27N3O4 |
| Formula Wt. | 361.44 |
| IUPAC Name | (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; LY450139; LY 450139 |
| Solubility | DMSO 72 mg/mL (199.2 mM) Ethanol 41 mg/mL (113.43 mM) Water Insoluble |
| Appearance | White to off white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Beggiato S, Giuliani A, Sivilia S, et al. CHF5074 and LY450139 sub-acute treatments differently affect cortical extracellular glutamate levels in pre-plaque Tg2576 mice. Neuroscience. 2014 Apr 25;266:13-22. PMID: 24530449.
Doody RS, Raman R, Farlow M, et al. A phase 3 trial of semagacestat for treatment of Alzheimer's disease. N Engl J Med. 2013 Jul 25;369(4):341-50. PMID: 23883379.
Schellekens H, McNamara O, Dinan TG, et al. Semagacestat, a γ-secretase inhibitor, activates the growth hormone secretagogue (GHS-R1a) receptor. J Pharm Pharmacol. 2013 Apr;65(4):528-38. PMID: 23488781.