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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-SB-399885
SB-399885

Chemical Structure : SB-399885

CAS No.: 402713-80-8

SB-399885 (SB399885)

货号: PC-63483Not For Human Use, Lab Use Only.

SB-399885 is a potent, selective, brain penetrant 5-HT6 receptor antagonist with pKi of 9.11 and 9.02 for human recombinant and native 5-HT6 receptors.

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10 mg ¥1280 In stock
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50 mg ¥3580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SB-399885 is a potent, selective, brain penetrant 5-HT6 receptor antagonist with pKi of 9.11 and 9.02 for human recombinant and native 5-HT6 receptors.
SB-399885 is a potent competitive antagonist (pA(2)=7.85), displays over 200-fold selectivity over other receptors.
SB-399885 significantly increases extracellular acetylcholine levels in rat medial prefrontal cortex, exhibits cognitive enhancing properties in recognition models.
SB-399885 also is an inhibitor of HCV entry in liver-derived cell lines as well as primary hepatocytes, modulates localization of the coreceptor tight junction protein claudin-1 (CLDN1) in a 5-HT6-independent manner, induces intracellular accumulation of CLDN1.

物理化学性质&存储条件

分子量 446.343
分子式 C18H21Cl2N3O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3,5-dichloro-2-methoxyphenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide

参考文献

1. Wesołowska A, et al. Eur J Pharmacol. 2008 Mar 17;582(1-3):88-93.

2. Riva L, et al. J Virol. 2018 Apr 27;92(10). pii: e01982-17.

3. Hirst WD, et al. Eur J Pharmacol. 2006 Dec 28;553(1-3):109-19.

4. Wesołowska A, et al. Neuropharmacology. 2007 Apr;52(5):1274-83.

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