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Submit ReviewSB 258585 hydrochloride
说明： Potent, selective 5-HT6 antagonist
化学名： 4-Iodo-N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]benzenesulfonamide hydrochloride
纯度： ≥98% (HPLC)
生物活性 for SB 258585 hydrochloride
SB 258585 hydrochloride is a potent and selective 5-HT6 receptor antagonist (pKi = 8.6); displays > 160-fold selectivity over other 5-HT receptor subtypes.
许可信息
Sold for research purposes under agreement from GlaxoSmithKline
技术数据 for SB 258585 hydrochloride
| 分子量 | 523.82 |
| 公式 | C18H22IN3O3S.HCl |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1216468-02-8 |
| PubChem ID | 53429667 |
| InChI Key | BFGOZFXMAJBFGI-UHFFFAOYSA-N |
| Smiles | Cl.COC1=CC=C(NS(=O)(=O)C2=CC=C(I)C=C2)C=C1N1CCN(C)CC1 |
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 SB 258585 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 5.24 | 10 | |
| DMSO | 26.19 | 50 |
制备储备液 for SB 258585 hydrochloride
以下数据基于产品分子量 523.82。 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 |
|---|---|---|---|
| 0.5 mM | 3.82 mL | 19.09 mL | 38.18 mL |
| 2.5 mM | 0.76 mL | 3.82 mL | 7.64 mL |
| 5 mM | 0.38 mL | 1.91 mL | 3.82 mL |
| 25 mM | 0.08 mL | 0.38 mL | 0.76 mL |
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产品说明书 for SB 258585 hydrochloride
参考文献 for SB 258585 hydrochloride
参考文献是支持产品生物活性的出版物。
Bromidge et al (1999) 5-Chloro-N-(4-methoxy-3-piperazin-1-yl-phenyl)-3-methyl-2-benzothiophenesulfonamide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist. J.Med.Chem. 42 202 PMID: 9925723
East et al (2002) 5-HT6 receptor binding sites in schizophrenia and following antipsychotic drug administration: autoradiographic studies with [125I]SB-258585. Synapse 45 191 PMID: 12112397
Hirst et al (2000) Characterization of [125I]-SB-258585 binding to human recombinant and native 5-HT6 receptors in rat, pig and human brain tissue. Br.J.Pharmacol. 130 1597 PMID: 10928963
If you know of a relevant reference for SB 258585 hydrochloride, please let us know.
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关键词: SB 258585 hydrochloride, SB 258585 hydrochloride supplier, Potent, selective, 5-HT6, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, SB258585, hydrochloride, GlaxoSmithKline, GSK, 1961, Tocris Bioscience
3 篇 SB 258585 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SB 258585 hydrochloride 的部分引用包括：
Yun et al (2016) Peripheral serotonin-mediated system suppresses bone development and regeneration via serotonin 6 G-protein-coupled receptor. Scientific Reports 6 30985 PMID: 27581523
Sun et al (2018) Activation and blockade of basolateral amygdala 5-HT6 receptor produce anxiolytic-like behaviors in an experimental model of Parkinson's disease. Neuropharmacology 137 275 PMID: 29778944
Hampson et al (2007) Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs. Diabetologia 50 1743 PMID: 17579833
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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.
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Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.