| 中文名称 |
PQR626
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| 英文名称 |
PQR626
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| 英文别名 |
mTOR inhibitor-7;PQR626;NSC828318
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| Cas No. |
1927857-98-4
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| 分子式 |
C20H27F2N7O2
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| 分子量 |
435.47
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| 包装储存 |
Powder -20°C 3 years;4°C 2 years
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| 详情描述 |
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 Ki 的值分别为 5 nM 和 3.6 nM。PQR626 可用于神经系统疾病的研究。
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| 产品详情 |
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 Ki 的值分别为 5 nM 和 3.6 nM。PQR626 可用于神经系统疾病的研究。
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| 生物活性 |
PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC 50 and K i of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
IC50: 5 nM (mTOR)
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| 体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis-
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| 体内研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years;4°C 2 years
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| 参考文献 |
[1]. Denise RAGEOT, et al. Treatment of neurological disorders. WO2017198346A1.[2]. Chiara Borsari, et al. 4-(Difluoromethyl)-5-(4-((3 R,5 S)-3,5-dimethylmorpholino)-6-(( R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Dis
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| 溶解度数据 |
In Vitro: DMSO : 100 mg/mL (229.64 mM; Need ultrasonic)配制储备液
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[1]. Denise RAGEOT, et al. Treatment of neurological disorders. WO2017198346A1.[2]. Chiara Borsari, et al. 4-(Difluoromethyl)-5-(4-((3 R,5 S)-3,5-dimethylmorpholino)-6-(( R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Dis
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。