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BMS-708163 (Avagacestat) is a potent, selective γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, respectively. BMS-708163 binds directly to the presenilin-1 N-terminal fragment and that binding can be challenged by other pan-GSIs, but not by γ-secretase modulators. BMS-708163 blocks the binding of four different active site-directed GSI photoaffinity probes. Administration of a single dose of 200 or 400 mg of BMS-708163 resulted in a marked decrease in CSF Aβ(1-38), Aβ(1-40) and Aβ(1-42) concentrations vs placebo; with smaller decreases observed in the 50 mg dose group. BMS-708163 (Avagacestat) was quickly absorbed into the systemic circulation, with a mean time to reach maximum plasma concentration (t(max)) of approximately 1-2 h, and a CSF t(max) of approximately 3 h. BMS-708163 is 190-fold more selective for APP than Notch, having an IC50 of 58 nM for Notch.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Harlan Sprague Dawley rat or ATM-405-142K9 naive II dog |
| Formulation | 99% PEG-400, 1% Tween-80 (rat)，or 94% labrafil-1944, 5% ethanol, 1% Tween-80 (dog) |
| Dosages | 10 mg/kg (rat) or 2.5 mg/kg (dog) |
| Administration | oral gavage |
| Molecular Weight | 520.88 |
| Formula | C20H17ClF4N4O4S |
| CAS Number | 1146699-66-2 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Crump CJ, et al. Biochemistry. BMS-708,163 targets presenilin and lacks notch-sparing activity.
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