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Submit ReviewPF 04479745
说明： Potent and selective 5-HT2C agonist
化学名： (9S)-6,7,8,9-Tetrahydro-N,9-dimethyl-2-(phenylmethyl)-5H-pyrimido[4,5-d]azepin-4-amine
纯度： ≥98% (HPLC)
生物活性 for PF 04479745
PF 04479745 is a potent and selective 5-HT2C agonist (EC50 = 10 nM). Exhibits > 100-fold selectivity over a panel of 90 receptors, enzymes and ion channels, except for 5-HT2A (IC50 = 360 nM antagonist), 5-HT2B (EC50 = 67 nM antagonist), 5-HT1A and 5-HT6 (functional activity not tested).
许可信息
Sold for research purposes under agreement from Pfizer Inc.
化合物库 for PF 04479745
PF 04479745 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for PF 04479745
| 分子量 | 282.39 |
| 公式 | C17H22N4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1065110-43-1 |
| PubChem ID | 90644511 |
| InChI Key | IHHALLDEDARSAL-LBPRGKRZSA-N |
| Smiles | C[C@@H]1C2=NC(CC3=CC=CC=C3)=NC(NC)=C2CCNC1 |
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.
溶解性数据 for PF 04479745
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 28.24 | 100 | |
| ethanol | 28.24 | 100 |
制备储备液 for PF 04479745
以下数据基于产品分子量 282.39。 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 | 3.54 mL | 17.71 mL | 35.41 mL |
| 5 mM | 0.71 mL | 3.54 mL | 7.08 mL |
| 10 mM | 0.35 mL | 1.77 mL | 3.54 mL |
| 50 mM | 0.07 mL | 0.35 mL | 0.71 mL |
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产品说明书 for PF 04479745
参考文献 for PF 04479745
参考文献是支持产品生物活性的出版物。
Storer et al (2014) Multiparameter optimization in CNS drug discovery: Design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT2C) receptor agonists with exquisite functional selectivity over 5-HT2A and 5-HT2B receptors. J.Med.Chem. 57 5258 PMID: 24878222
If you know of a relevant reference for PF 04479745, please let us know.
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关键词: PF 04479745, PF 04479745 supplier, PF04479745, potent, selective, 5-hydroxytryptamine, 2C, 5-HT2C, agonists, agonism, Receptors, 5755, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.