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Submit ReviewDR 4485 hydrochloride
说明： High affinity and selective 5-HT7 antagonist; orally bioavailable
化学名： 6-Chloro-2a-[4-[4-(4-chlorophenyl)-3,6-dihydro-1(2H)-pyridinyl]butyl]-2a,3,4,5-tetrahydrobenz[cd]indol-2(1H)-one hydrochloride
纯度： ≥98% (HPLC)
生物活性 for DR 4485 hydrochloride
DR 4485 hydrochloride is a high affinity and selective 5-HT7 antagonist (pKi = 8.14). Exhibits selectivity for 5-HT7 over other 5-HT receptors. Inhibits 5-HT-induced cAMP accumulation in HEK-293 cells expressing the 5-HT7 receptor. Orally bioavailable.
化合物库 for DR 4485 hydrochloride
DR 4485 hydrochloride 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 DR 4485 hydrochloride
| 分子量 | 491.88 |
| 公式 | C26H28Cl2N2O.HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 402942-53-4 |
| PubChem ID | 90488996 |
| InChI Key | QAERYGXKDZHTFR-UHFFFAOYSA-N |
| Smiles | ClC1=C2C(C3(CCCCN4CCC(C5=CC=C(Cl)C=C5)=CC4)CCC2)=C(NC3=O)C=C1.Cl |
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 DR 4485 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 49.19 | 100 |
制备储备液 for DR 4485 hydrochloride
以下数据基于产品分子量 491.88。 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 | 2.03 mL | 10.17 mL | 20.33 mL |
| 5 mM | 0.41 mL | 2.03 mL | 4.07 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.03 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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产品说明书 for DR 4485 hydrochloride
参考文献 for DR 4485 hydrochloride
参考文献是支持产品生物活性的出版物。
Kikuchi et al (2003) New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability. Bioorg.Med.Chem.Lett. 13 61 PMID: 12467617
Medina et al (2009) Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity. J.Med.Chem. 52 2384 PMID: 19326916
If you know of a relevant reference for DR 4485 hydrochloride, please let us know.
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关键词: DR 4485 hydrochloride, DR 4485 hydrochloride supplier, DR4485, hydrochloride, high, affinity, potent, 5-HT-7, selective, serotonin, orally, bioavailable, antagonists, 5-HT7, Receptors, 5005, Tocris Bioscience
3 篇 DR 4485 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 DR 4485 hydrochloride 的部分引用包括：
Gerd et al (2021) Autophagy activation, lipotoxicity and lysosomal membrane permeabilization synergize to promote pimozide- and loperamide-induced glioma cell death. Autophagy 17 3424-3443 PMID: 33461384
Chan et al (2016) A Miniaturized Screen of a Schistosoma mansoni Serotonergic G Protein-Coupled Receptor Identifies Novel Classes of Parasite-Selective Inhibitors. PLoS Pathog 12 e1005651 PMID: 27187180
Thomas C et al (2019) Neuromodulator Signaling Bidirectionally Controls Vesicle Numbers in Human Synapses. Cell 179 498-513.e22 PMID: 31585084
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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.