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Submit ReviewSB 271046 hydrochloride
说明： Selective 5-HT6 antagonist; orally active
化学名： 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-benzo[b]thiophen-2-sulfonamide hydrochloride
纯度： ≥99% (HPLC)
生物活性 for SB 271046 hydrochloride
SB 271046 hydrochloride is a selective, orally active 5-HT6 antagonist (pKi values are 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. Increases extracellular glutamate and aspartate in the frontal cortex, and exhibits anticonvulsant activity (EC50 = 0.16 μM).
许可信息
Sold with the permission of GlaxoSmithKline
化合物库 for SB 271046 hydrochloride
SB 271046 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 SB 271046 hydrochloride
| 分子量 | 488.45 |
| 公式 | C20H22ClN3O3S2.HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 209481-24-3 |
| PubChem ID | 6918455 |
| InChI Key | RMXZRJYGJMSDQK-UHFFFAOYSA-N |
| Smiles | CC2=C(S(NC3=CC=C(OC)C(N4CCNCC4)=C3)(=O)=O)SC1=CC=C(Cl)C=C12.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 SB 271046 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 48.84 | 100 |
制备储备液 for SB 271046 hydrochloride
以下数据基于产品分子量 488.45。 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 | 2.05 mL | 10.24 mL | 20.47 mL |
| 5 mM | 0.41 mL | 2.05 mL | 4.09 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.05 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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产品说明书 for SB 271046 hydrochloride
参考文献 for SB 271046 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
Dawson et al (2000) In vivo effects of the 5-HT6 antagonist SB-271046 on striatal and frontal cortex extracellular concentrations of noradrenaline, DA, 5-HT, glutamate and aspartate. Br.J.Pharmacol. 130 23 PMID: 10780993
Routledge et al (2000) Characterization of SB-271046: a potent, selective and orally active 5-HT6 receptor antagonist. Br.J.Pharmacol. 130 1606 PMID: 10928964
Marcos et al (2008) Effects of 5-HT6 receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat. Br.J.Pharmacol. 155 434 PMID: 18622410
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关键词: SB 271046 hydrochloride, SB 271046 hydrochloride supplier, Orally, active, selective, 5-HT6, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, SB271046, hydrochloride, GlaxoSmithKline, GSK, 3368, Tocris Bioscience
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