BPN-15606 是一种高效的口服活性 γ-secretase 调节剂 (GSM)，可减弱 SHSY5Y 神经母细胞瘤细胞产生 Aβ42 和 Aβ40 的作用，IC₅₀ 值分别为 7 nM 和 17 nM。BPN-15606 可以降低大鼠和小鼠中枢神经系统中的 Aβ42 和 Aβ40 水平。BPN-15606 具有良好的 PK/PD 特性，包括生物利用度，半衰期和清除率。

BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC 50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.

Solid

γ-secretase

BPN-15606 (oral administration; 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 (oral administration; 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 (oral administration; 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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[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.

In Vitro: DMSO : 100 mg/mL (238.97 mM; Need ultrasonic)配制储备液