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BPN-15606 besylate is a potent, orally active γ-secretase regulator (GSM) that reduces the production of Aβ42 (IC50: 7 nM) and Aβ40 (IC50: 17 nM) by SHSY5Y neuroblastoma cells. BPN-15606 besylate exhibited good PK/PD properties (including bioavailability, half-life and clearance).