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PQR626

CAS No. : 1927857-98-4

MCE 站：PQR626

产品活性：PQR626 是一种雷帕霉素类似物。PQR626 是一种高效的，选择性的，具有口服活性的，能穿过血脑屏障的 mTOR 抑制剂，其 IC₅₀ 和 K_i 的值分别为 5 nM 和 3.6 nM。PQR626 可用于神经系统疾病的研究。

研究领域：PI3K/Akt/mTOR

作用靶点：mTOR

In Vitro: PQR626 (0.04-5 μΜ; 1 hour) has IC₅₀s of 197 nM and 87 nM for pPKB S473 and pS6 S235/S236, respectively, in-cell western blot. S6 kinase (S6K), S6 ribosomal protein (S6rP) and 4E-binding protein (4E-BP) are prominent downstream effectors of mTOR.

In Vivo: PQR626 (10-50 mg/kg; twice a day; for 90 days) reduces the loss of Tsc1-induced mortality as compared to vehicle.
PQR626 exhibits terminal elimination half-life (mice 3.0 h) due to high plasma clearance (1096 ng/mL) following oral dosing (10 mg/kg; p.o.; daily; for 4 days).

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