BMS-708163 (Avagacestat) is a potent and selective inhibitor for gamma-secretase, especially at inhibiting cleavage of amyloid precursor protein (APP) to form amyloid-ß (Aß)(1-40) (IC50=0.3nM) and Aß(1-42) (0.27nM). BMS-708163 is ??Notch sparing??, with more than 100 folds more selective for APP than for Notch protein (IC50 of 58nM).

BMS-708163 is developed for treating Alzheimer??s disease (AD). Oral administration of BMS-708163 significantly reduced Aß(1-40) levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs [1]. The results of Phase II clinical trial in mild-to-moderate AD patients demonstrated acceptable tolerability at a single-dose range of 0.3 to 800 mg with a biphasic effect on plasma Aß(1-40) [2].

Technical information:

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution at -20^oC.

Reference:

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.