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PHA 568487 free base {[allProObj[0].p_purity_real_show]}

货号:A1174872

PHA 568487 is agonist of the α7 nicotinic acetylcholine receptor with Ki value of 44.

PHA 568487 free base 化学结构 CAS号:527680-56-4
PHA 568487 free base 化学结构
CAS号:527680-56-4
PHA 568487 free base 3D分子结构
CAS号:527680-56-4
PHA 568487 free base 化学结构 CAS号:527680-56-4
PHA 568487 free base 3D分子结构 CAS号:527680-56-4
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PHA 568487 free base 纯度/质量文件 产品仅供科研

货号:A1174872 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AChE AChR mAChR nAChR 其他靶点 纯度
Donepezil +++

bAChE, IC50: 8.12 nM

hAChE, IC50: 11.6 nM

98%
Loganin ++

AChE, IC50: 3.95 μM

99%+
topride HCl ++

AChE, IC50: 2.04 μM

98%
Dehydroevodiamine HCl 99%+
Jatrorrhizine ++

AChE, IC50: 872 nM

99%+
Palmatine ++

AChE, IC50: 0.51 μM

95%
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

98%
Galanthamine HBr ++

AChE, IC50: 0.35 μM

98%
Trospium chloride 99%
Tiotropium Bromide Monohydrate 97%
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

98%
Hexamethonium Bromide 99%
Pancuronium dibromide 98%
Neostigmine bromide 98%
Orphenadrine citrate 98%
Oxybutynin 98%
Irsogladine PDE 99%
Pyridostigmine bromide 99+%
Rivastigmine +

AChR, IC50: 5.5 μM

98%
Paroxetine HCl 99%
Rocuronium Bromide 98%
Tropicamide +++

M4 mAChR, IC50: 8 nM

98%
Diphenmanil methylsulfate 99%
Umeclidinium bromide 95%
Otilonium bromide 98%
Flavoxate HCl +

mAChR, IC50: 12.2 μM

99%
Ipratropium bromide 98%
Diphenidol HCl 98%
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

98%
Aclidinium Bromide ++++

M2 mAChR, Ki: 0.1 nM

M4 mAChR, Ki: 0.21 nM

98%
Oxybutynin chloride 99%
Pentoxyverine citrate 98%
Solifenacin 98%
Catharanthine 98%
Benzethonium chloride +++

α4β2 nAChRs, IC50: 49 nM

α7 nAChRs, IC50: 122 nM

99+%
Vinblastine sulfate +

nAChR, IC50: 8.9 μM

99%
PNU-120596 ++

α7 nAChR, EC50: 216 nM

99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

PHA 568487 free base 生物活性

描述 PHA 568487 free base acts as a selective agonist for the alpha 7 nicotinic acetylcholine receptor (α-7 nAchR). It attenuates neuroinflammation[1][2][3].

PHA 568487 free base 动物研究

Animal study PHA 568487 Treatment mitigates cognitive decline in mice induced by aseptic bone fracture through the promotion of inflammation resolution. PHA 568487 (PHA; 0.8 mg/kg; administered intraperitoneally) decreases infarct volume and the presence of TUNEL-positive neurons in the peri-infarct regions of permanent middle cerebral artery occlusion (pMCAO) and pMCAO+tibia fracture mice[2].The involvement of α7 receptors in neuroinflammation is evidenced by the reduction in [18F]DPA-714 binding observed in ischemic rats treated with the α7 agonist PHA 568487 at day 7 post-MCAO[3].Ischemic rats treated with PHA 568487 exhibit a notable decrease in cerebral infarct volumes and an enhancement in neurological outcomes compared to MCAO rats that were not treated[3].

PHA 568487 free base 参考文献

[1]F Barclay Shilliday, et al. Multiple species metabolism of PHA-568487, a selective alpha 7 nicotinic acetylcholine receptor agonist. Drug Metab Lett. 2010 Aug;4(3):162-72.

[2]Zhenying Han, et al. Alpha-7 nicotinic acetylcholine receptor agonist treatment reduces neuroinflammation, oxidative stress, and brain injury in mice with ischemic stroke and bone fracture. J Neurochem. 2014 Nov;131(4):498-508.

[3]Lorena Colás, et al. In vivo imaging of Α7 nicotinic receptors as a novel method to monitor neuroinflammation after cerebral ischemia. Glia. 2018 Aug;66(8):1611-1624.

PHA 568487 free base 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.47mL

0.69mL

0.35mL

17.34mL

3.47mL

1.73mL

34.68mL

6.94mL

3.47mL

PHA 568487 free base 技术信息

CAS号527680-56-4
分子式C16H20N2O3
分子量 288.34
SMILES Code O=C(C1=CC=C(OCCO2)C2=C1)N[C@H]3CN4CCC3CC4
MDL No. MFCD11519961
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
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