产品
编 号:F621449
分子式:C20H27F2N7O2
分子量:435.47
产品类型
结构图
CAS No: 1927857-98-4
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产品详情
生物活性:
PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC50 and Ki of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders.
体内研究:
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).Animal Model:BALB/c nude female mice, Tsc1GFAP CKO mice model
Dosage:10 mg/kg, 25 mg/kg, 50 mg/kg
Administration:Oral administration, twice a day, for 90 days
Result:Significantly reduced the loss of Tsc1-induced mortality.
Animal Model:Female C57BL/6J Mice
Dosage:10 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration, daily, for 4 days
Result:Cmax (1096 ng/mL), T1/2 (3.0 h).
体外研究:
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.