生物活性 | BPN-15606 besylate is a highly potent, orally activeγ-secretasemodulator (GSM), attenuates the production ofAβ42andAβ40by SHSY5Y neuroblastoma cells withIC50values 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[1]. |
IC50& Target | γ-secretase[1] |
体外研究 (In Vitro) | 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[1].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[1].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[1]. |
分子量 | 576.64 |
Formula | C29H29FN6O4S |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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