Research Article
Modulation of Gamma-Secretase for the Treatment of Alzheimer's Disease
Table 2
GSM potency versus plasma exposure in mice.
| | E-2012 | JNJ-40418677 | GSM1 | SPI-1810 |
| In vitro A IC50 (nM) CHO-2B7 cells | 33 | 172 | 62 | 114 | Plasma exposure (M) | 4923 | 7764 | 2744 | 14638 | Plasma fold over A IC50 for 25% reduction | 149 | 45 | 44 | 128 | Brain exposure (M) | 2749 | 7497 | 8681 | 20368 | Brain fold over A IC50 for 25% reduction | 83 | 44 | 140 | 179 |
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