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编 号:F752731
分子式:C29H29FN6O4S
分子量:576.64
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生物活性:
BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.

体外研究:
BPN-15606 besylate (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 besylate (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 besylate (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.
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