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Submit ReviewPHA 568487 is an agonist of the α7 nicotinic acetylcholine receptor (Ki values are 44 and 2800 for α7 and 5-HT3 respectively, IC50 values are > 100 μM for α3β4 and α1β1δγ respectively, and % inhibition is < 1 and 5% for α4β2 and hERG respectively). Orally active and brain penetrant.
PHA 568487 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 404.41 |
公式 | C16H20N2O3.C4H4O4 |
储存 | Desiccate at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 527680-57-5 |
PubChem ID | 56972212 |
InChI Key | QYQZUGYJVHHHEE-QDSMGTAFSA-N |
Smiles | O=C(C3=CC=C(OCCO4)C4=C3)N[C@@H]1C2CCN(CC2)C1.O=C(/C=C/C(O)=O)O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 40.44 | 100 | |
DMSO | 40.44 | 100 |
以下数据基于产品分子量 404.41。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.47 mL | 12.36 mL | 24.73 mL |
5 mM | 0.49 mL | 2.47 mL | 4.95 mL |
10 mM | 0.25 mL | 1.24 mL | 2.47 mL |
50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
参考文献是支持产品生物活性的出版物。
Walker et al (2006) Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as α7 nicotinic acetylcholine receptor agonists. Bioorg.Med.Chem. 14 8219 PMID: 17011782
If you know of a relevant reference for PHA 568487, please let us know.
关键词: PHA 568487, PHA 568487 supplier, α7, alpha7, selective, agonists, a7, Nicotinic, Receptors, Acetylcholine, nAChR, PHA568487, (a7), 3134, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PHA 568487 的部分引用包括:
Foucault-Fruchard (2017) Neuroprotective effect of the alpha 7 nicotinic receptor agonist PHA 543613 in an n vivo excitotoxic adult rat model. Neuroscience 356 52 PMID: 28527955
Su et al (2013) Dysfunction of inflammation-resolving pathways is associated with exaggerated postoperative cognitive decline in a rat model of the metabolic syndrome. Mol Med 18 1481 PMID: 23296426
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