PQR626|cas:1927857-98-4|西域试剂

PQR626,98.02%

产品编号：Bellancom-136660| CAS NO：1927857-98-4| 分子式：C₂₀H₂₇F₂N₇O₂| 分子量：435.47

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-136660	￥4100.00	杭州北京（现货）
Bellancom-136660	￥7100.00	杭州北京（现货）
Bellancom-136660	￥11000.00	杭州北京（现货）
Bellancom-136660	￥20000.00	杭州北京（现货）
Bellancom-136660	￥31000.00	杭州北京（现货）

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PQR626

产品介绍

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。

生物活性

PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC₅₀ and K_i of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c nude female mice, Tsc1^GFAP 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:	C_max (1096 ng/mL), T_1/2 (3.0 h).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c nude female mice, Tsc1^GFAP 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:	C_max (1096 ng/mL), T_1/2 (3.0 h).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c nude female mice, Tsc1^GFAP 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:	C_max (1096 ng/mL), T_1/2 (3.0 h).

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (229.64 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2964 mL	11.4818 mL	22.9637 mL
5 mM	0.4593 mL	2.2964 mL	4.5927 mL
10 mM	0.2296 mL	1.1482 mL	2.2964 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式