| Description | BPN-15606 besylate is a highly potent, orally active γ-secretase modulator, attenuates the production of Aβ40 and Aβ42 by SHSY5Y neuroblastoma cells (IC50s: 7 nM and 17nM). |
| In vivo | BPN-15606 besylate (p.o.; 10 mg/kg, 25 mg/kg, and 50 mg/kg; 7 days) shows excellent dose-dependent efficacy in both plasma and brain on lowering of Aβ42 and Aβ40 levels in mice. BPN-15606 besylate (p.o.; 5 mg/kg, 25 mg/kg and 50 mg/kg; 9 days) dose-dependently reduces CSF on lowering of Aβ42 and Aβ40 levels in rats. BPN-15606 besylate (p.o.; 25 mg/kg; single dose) shows a robust effect on both brain and plasma Aβ 42 and Aβ40 levels, which begins approximately 30–60 minutes following the single-dose administration and lasted for ≥24 hours in C57BL/6 mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance. |
| Synonyms | BPN-15606 besylate |
| molecular weight | 576.64 |
| Molecular formula | C29H29FN6O4S |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Wagner SL, et al. Pharmacological and Toxicological Properties of the Potent Oral γ-Secretase Modulator BPN-15606. J Pharmacol Exp Ther. 2017 Jul;362(1):31-44. |