| 名称 | PQR626 |
| 描述 | PQR626 is a rapamycin derivative that acts as a highly potent, selective, orally active, and brain-penetrant mTOR inhibitor. It exhibits remarkable inhibitory effects on the mammalian target of the rapamycin (mTOR) pathway, with an IC50 value of 5 nM and a Ki value of 3.6 nM. This compound, PQR626, holds promise for advancing research in the field of neurological disorders. |
| 体外活性 | PQR626 (0.04-5 μΜ; 1 hour) has IC 50 s 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[1]. Western Blot Analysis[1]Cell Line: A2058 cells Concentration: 0.04 μΜ, 0.08 μΜ, 0.155 μΜ, 0.3125 μΜ, 0.625 μΜ, 1.25 μΜ, 5 μΜ Incubation Time: 1 hour Result: Inhibited mTOR in cell. |
| 体内活性 | PQR626 (10-50 mg/kg; twice a day; for 90 days) reduces the loss of Tsc1 -induced mortality as compared to vehicle[2]. 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)[2]. Animal Model: BALB/c nude female mice, Tsc1 GFAP CKO mice model[2]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[1]Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration, daily, for 4 days Result: C max (1096 ng/mL), T 1/2 (3.0 h). |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 关键字 | PQR-626 | PQR 626 |
| 相关产品 | L-Proline | Metformin | Rapamycin | Resveratrol | Methyl eugenol | L-Leucine | (E/Z)-10-Hydroxy-2-decenoic acid | Dihydromyricetin | N-Hydroxyphthalimide | Metformin hydrochloride | Stearamide | 4-Vinylcyclohexene Dioxide |
