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SB742457,且5-HT6拮抗剂, 羟色胺 6（5-HT6）受体拮抗剂

高效且高度选择性的5-HT6拮抗剂
规格或纯度: ≥97%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
S127746-1mg
 1mg 现货 Stock Image
S127746-5mg
 5mg 现货 Stock Image
S127746-25mg
 25mg 现货 Stock Image
S127746-100mg
 100mg 期货 Stock Image
大包装询价 添加到收藏夹 比较  SDS中文版  DATASHEET
main product photo

基本描述

英文别名 Intepirdine|607742-69-8|SB-742457|SB742457|GSK-742457|SB 742457|3-(PHENYLSULFONYL)-8-(PIPERAZIN-1-YL)QUINOLINE|RVT-101|Quinoline, 3-(phenylsulfonyl)-8-(1-piperazinyl)-|3-Phenylsulfonyl-8-(piperazin-1-yl)quinoline|GSK 742457|2IOB2M82HY|CHEMBL1083390|3-(ben
规格或纯度 ≥97%
英文名称 SB742457
生化机理 SB-742457, a 5-HT6 receptor antagonist, which extends into Alzheimer disease (AD) sufferers further highlights the therapeutic promise of this mechanistic approach. Alzheimer's disease is a devastating neurological condition characterized by a progressive decline in cognitive performance accompanied by behavioral and psychological syndromes, such as depression and psychosis. With the subsequent development of selective 5-HT6 receptor antagonists, preclinical studies in rodents and primates have elucidated the function of this receptor subtype in more detail. It is increasingly clear that blockade of 5-HT6 receptors leads to an improvement of cognitive performance in a wide variety of learning and memory paradigms and also results in anxiolytic and antidepressant-like activity. SB-742457 is generally safe and well tolerated and may be efficacious in Alzheimer disease.Potent (pKi = 9.63) and highly selective 5-HT6 antagonist. Greater thsan 100-fold selective against other receptors. Reverses learning impairment in animal models.
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。有毒，请参阅SDS以获取更多信息。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍

SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.

SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.

产品属性

ALogP 2.5

名称和标识符

IUPAC Name 3-(benzenesulfonyl)-8-piperazin-1-ylquinoline
INCHI InChI=1S/C19H19N3O2S/c23-25(24,16-6-2-1-3-7-16)17-13-15-5-4-8-18(19(15)21-14-17)22-11-9-20-10-12-22/h1-8,13-14,20H,9-12H2
InChi Key JJZFWROHYSMCMU-UHFFFAOYSA-N
Canonical SMILES C1CN(CCN1)C2=CC=CC3=CC(=CN=C32)S(=O)(=O)C4=CC=CC=C4
Isomeric SMILES C1CN(CCN1)C2=CC=CC3=CC(=CN=C32)S(=O)(=O)C4=CC=CC=C4
PubChem CID 11256720
分子量 353.44

化学和物理性质

溶解性 DMSO 78 mg/mL Water <1 mg/mL Ethanol 2 mg/mL

安全和危险性（GHS）

象形图
ghs06

Toxic
信号词 Danger
危险声明 H301: Toxic if swallowed
预防措施声明 P321,P405,P501,P264,P270,P330,P301+P316

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参考文献

1. Liu KG, Lo JR, Comery TA, Zhang GM, Zhang JY, Kowal DM, Smith DL, Di L, Kerns EH, Schechter LE et al..  (2009)  Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands..  Bioorg Med Chem Lett,  19  (12):  (3214-6).  [PMID:19433358]
2. Maher-Edwards G, Zvartau-Hind M, Hunter AJ, Gold M, Hopton G, Jacobs G, Davy M, Williams P.  (2010)  Double-blind, controlled phase II study of a 5-HT6 receptor antagonist, SB-742457, in Alzheimer's disease..  Curr Alzheimer Res,  7  (5):  (374-85).  [PMID:20043816]
3. Maher-Edwards G, Dixon R, Hunter J, Gold M, Hopton G, Jacobs G, Hunter J, Williams P.  (2011)  SB-742457 and donepezil in Alzheimer disease: a randomized, placebo-controlled study..  Int J Geriatr Psychiatry,  26  (5):  (536-44).  [PMID:20872778]
4. Callaghan CK, Hok V, Della-Chiesa A, Virley DJ, Upton N, O'Mara SM.  (2012)  Age-related declines in delayed non-match-to-sample performance (DNMS) are reversed by the novel 5HT6 receptor antagonist SB742457..  Neuropharmacology,  63  (5):  (890-7).  [PMID:22766392]
5. Ferrero H, Solas M, Francis PT, Ramirez MJ.  (2017)  Serotonin 5-HT6 Receptor Antagonists in Alzheimer's Disease: Therapeutic Rationale and Current Development Status..  CNS Drugs,  31  (1):  (19-32).  [PMID:27914038]
6. Rossé G, Schaffhauser H.  (2010)  5-HT6 receptor antagonists as potential therapeutics for cognitive impairment..  Curr Top Med Chem,  10  (2):  (207-21).  [PMID:20166958]
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