PF-06447475|cas:1527473-33-1|西域试剂

PF-06447475,99.94%

产品编号：Bellancom-12477| CAS NO：1527473-33-1| 分子式：C₁₇H₁₅N₅O| 分子量：305.33

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-12477	￥550.00	杭州北京（现货）
Bellancom-12477	￥800.00	杭州北京（现货）
Bellancom-12477	￥1600.00	杭州北京（现货）
Bellancom-12477	￥2400.00	杭州北京（现货）
Bellancom-12477	￥3600.00	杭州北京（现货）

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PF-06447475

产品介绍

PF-06447475是高效，选择性，能透过血脑屏障的 LRRK2 抑制剂，IC₅₀值为3 nM。

生物活性

PF-06447475 is a highly potent, selective and brain penetrant LRRK2 inhibitor with an IC₅₀ of 3 nM.

体外研究

PF-06447475 inhibits LRRK2 enzyme and LRRK2 in the whole cell assay with IC₅₀s of 3 and 25 nM, respectively. Cells incubated with PF-06447475 alone (0.5, 1, 3 μM) or in the presence of ROT significantly reduces (S935)-LRRK2 kinase phosphorylation to control. PF-06447475 significantly preserves the nucleus morphology and ΔΨm of NLCs exposed to ROT compared to untreated and control. PF-475 significantly diminishes ROT-induced ROS generation to a similar extent to cells exposed to PF-475 alone.

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

体内研究

In G2019S+ rats treated with PF-06447475, a significant reduction in microgliosis to levels found in wild-type rats could be observed. The proinflammatory marker MHC-II expressed on myeloid cells but not neurons also appears to be less abundant in confocal sections in G2019S+ rats treated with PF-06447475. PF-06447475 treatment in G2019S+ rats significantly lowers the number of CD68 cells recruited to the SNpc. PF-06447475 successfully blocks the enhanced neuroinflammation associated with G2019S-LRRK2 expression. Treatment of G2019S+ rats with PF-06447475 preserves TH expression in the dorsal striatum, consistent with drug attenuating neurodegeneration in the SNpc. PF-06447475 is well tolerated in rats.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 60 mg/mL (196.51 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2751 mL	16.3757 mL	32.7515 mL
5 mM	0.6550 mL	3.2751 mL	6.5503 mL
10 mM	0.3275 mL	1.6376 mL	3.2751 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 3 mg/mL (9.83 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (9.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 3 mg/mL (9.83 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (9.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。