Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 3,390 | 6-8周 | ||
25 mg | ¥ 12,700 | 6-8周 | ||
50 mg | ¥ 16,600 | 6-8周 | ||
100 mg | ¥ 25,800 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,750 | 6-8周 |
产品描述 | 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. |
靶点活性 | mTOR:5 nM (IC50) |
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). |
别名 | PQR626 |
分子量 | 435.48 |
分子式 | C20H27F2N7O2 |
CAS No. | 1927857-98-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PQR626 1927857-98-4 PQR-626 PQR 626 Inhibitor inhibitor inhibit