TABLE 1.
Isomeric IMT analogs are γ-secretase modulators a .
| Comp. ID | % Aβ38, 40, 42 of DMSO ctrl at 10 (5 µM) conc | Comp. ID | % Aβ38, 40, 42 of DMSO ctrl at 10 (5 µM) conc |
|---|---|---|---|
| 1a | 86, 40, 35 (105, 57, 49) | 1b | 61, 34, 33 (95, 56, 53) |
| 1d | 22, 14, 11 (60, 34, 28) | 1e | 91, 46, 44 (99, 57, 54) |
| 1f | 80, 29, 26 (113, 52, 45) | 1h | 80, 43, 43 (106, 64, 58) |
| 1i | 85, 41, 46 (106, 56, 58) | 1j | 123, 73, 65 (112, 83, 75) |
| 1k | 92, 38, 38 (120, 60, 56) | 1L | 52, 21, 17 (107, 48, 43) |
| 1n | 95, 42, 38 (112, 63, 56) | 1p | 24, 18, 15 (58, 41, 38) |
| 2b | 74, 71, 74 (93, 90, 88) |
a
The screening experiment was performed for Aβ40, 38 and 42 in cell supernatants of N2a695 cells using MSD ELISA., Drug concentrations are 10 μM or 5 μM. Aβ values are expressed as percentages of control Aβ38, 40, and 42, respectively. Results for the IMTi-1, derivatives shown here were obtained from a single experiment.