| 货号 | 16713-1mg |
| 描述 | γ-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and β-amyloid precursor protein (APP), within the transmembrane domain.1,2 Semagacestat is a potent inhibitor of γ-secretase that blocks the production of Aβ38, Aβ40, and Aβ42 with IC50 values of 12.0, 12.1, and 10.9 nM, respectively.3,4 It also blocks Notch signaling (IC50 = 14.1 nM).4 Semagacestat modulates γ-secretase activity in vivo, altering Aβ levels in brain, cerebrospinal fluids, and plasma in a dose-dependent fashion.3,4 Although semagacestat does not improve cognitive status in humans, it is useful as a pan γ-secretase inhibitor for research purposes.4,5 |
| 别名 | LY450139; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Andersson, E.R. and Lendahl, U. Therapeutic modulation of Notch signalling - are we there yet? Nature Reviews.Drug Discovery 13(5), 357-378 (2014). 2.Jurisch-Yaksi, N.,Sannerud, R. and Annaert, W. A fast growing spectrum of biological functions of γ-secretase in development and disease. Biochim Biophys.Acta. 1828(12), 2815-2827 (2013). 3.Lanz, T.A.,Karmilowicz, M.J.,Wood, K.M., et al. Concentration-dependent modulation of amyloid-β in vivo and in vitro using the γ-secretase inhibitor, LY-450139. Journal of Pharmacology and Experimental Therapeutics 319(2), 924-933 (2006). 4.Mitani, Y.,Yarimizu, J.,Saita, K., et al. Differential effects between γ-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice. Journal of Neuroscience 32(6), 2037-2050 (2012). 5.Doody, R.S.,Raman, R.,Farlow, M., et al. A phase 3 trial of semagacestat for treatment of Alzheimer’s disease. New England Journal of Medicine 369(4), 341-350 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 361.4 |
| 分子式 | C19H27N3O4 |
| CAS号 | 425386-60-3 |
| 稳定性 | ≥ 2 years |
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