PHA 568487 free base|cas:527680-56-4|西域试剂

PHA 568487 free base,99.52%

产品编号：Bellancom-129674| CAS NO：527680-56-4| 分子式：C₁₆H₂₀N₂O₃| 分子量：288.34

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货号	价格	库存与货期
Bellancom-129674	￥1200.00	杭州北京（现货）
Bellancom-129674	￥1980.00	杭州北京（现货）
Bellancom-129674	￥5950.00	杭州北京（现货）
Bellancom-129674	￥10500.00	杭州北京（现货）

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PHA 568487 free base

产品介绍

PHA 568487 free base 是一种选择性的 α 7 烟碱乙酰胆碱受体 (α-7 nAchR) 激动剂。PHA 568487 free base 可用于减缓神经炎症。

生物活性

PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation.

体外研究

PHA 568487, α-7 nAchR-specific agonist, prevents NF-κb activation in the cells.
PHA 568487 treatment significantly reduces the expression of leukocyte infiltration molecules in MCAO rats and in endothelial cells after in vitro ischemia.

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

体内研究

PHA 568487 treatment reduces mouse cognitive decline caused by aseptic bone fracture by promoting inflammation resolution. PHA 568487 (PHA; 0.8 mg/kg; injected intraperitoneally) reduces infarct volume and TUNEL positive neurons in the peri-infarct regions of permanent middle cerebral artery occlusion (pMCAO) and pMCAO+tibia fracture mice.
The role played by a7 receptors on neuroinflammation is supported by the decrease of [¹⁸F]DPA-714 binding in ischemic rats treated with the a7 agonist PHA 568487 at day 7 after MCAO.
PHA 568487-treated ischemic rats show a significant reduction of the cerebral infarct volumes and an improvement of the neurologic outcome compared with non-treated MCAO rats.

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

Animal Model:	C57BL/6J male mice (10-12 weeks old) with pMCAO
Dosage:	0.4 and 0.8 mg/kg
Administration:	Injected intraperitoneally once on day 1, or twice on days 1 and 2, after pMCAO
Result:	0.8 mg/kg on days 1 and 2 after pMCAO yielded the best effect on infarct volume and behavior tests.

Animal Model:	Adult male Sprague-Dawley rats
Dosage:	1.25 mg/kg
Administration:	Treated i.p. daily with 0.1 mL
Result:	Showed a significant decrease of [18F]DPA-714 binding in the ischemic cerebral hemisphere in comparison to non-treated ischemic rats.

体内研究

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

Animal Model:	C57BL/6J male mice (10-12 weeks old) with pMCAO
Dosage:	0.4 and 0.8 mg/kg
Administration:	Injected intraperitoneally once on day 1, or twice on days 1 and 2, after pMCAO
Result:	0.8 mg/kg on days 1 and 2 after pMCAO yielded the best effect on infarct volume and behavior tests.

Animal Model:	Adult male Sprague-Dawley rats
Dosage:	1.25 mg/kg
Administration:	Treated i.p. daily with 0.1 mL
Result:	Showed a significant decrease of [18F]DPA-714 binding in the ischemic cerebral hemisphere in comparison to non-treated ischemic rats.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (86.70 mM; ultrasonic and warming and adjust pH to 8 with HCl and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4681 mL	17.3406 mL	34.6813 mL
5 mM	0.6936 mL	3.4681 mL	6.9363 mL
10 mM	0.3468 mL	1.7341 mL	3.4681 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: ≥ 2.08 mg/mL (7.21 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.21 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (7.21 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.21 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (7.21 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.21 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。