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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-SB-271046
SB-271046

Chemical Structure : SB-271046

CAS No.: 209481-20-9

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SB-271046 (SB 271046 hydrochloride)

货号: PC-21121Not For Human Use, Lab Use Only.

SB-271046 is a potent, selective and orally active 5-HT6 receptor antagonist, potently displaces [(3)H]-LSD and [(125)I]-SB-258585 from human 5-HT6 receptors recombinantly expressed in HeLa cells with pKi 8.92 and 9.09 respectively.

规格 价格 库存 数量
10 mg ￥980 In stock
25 mg ￥1680 In stock
50 mg ￥2580 In stock
100 mg ￥4280 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SB-271046 is a potent, selective and orally active 5-HT6 receptor antagonist, potently displaces [(3)H]-LSD and [(125)I]-SB-258585 from human 5-HT6 receptors recombinantly expressed in HeLa cells with pKi 8.92 and 9.09 respectively.
SB-271046 also displaces [(125)I]-SB-258585 from human caudate putamen and rat and pig striatum membranes (pK(i) 8.81, 9.02 and 8.55 respectively).
SB-271046 is >200 fold selective for the 5-HT(6) receptor vs. 55 other receptors, binding sites and ion channels.
SB-271046 competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA(2) of 8.71 in functional studies on human 5-HT(6) receptors.
SB-271046 (10 mg/kg) demonstrates anticonvulsant activity in the rat MEST test.

物理化学性质&存储条件

分子量 488.44
分子式 C20H23Cl2N3O3S2
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

5-Chloro-3-methyl-benzo[b]thiophene-2-sulphonic acid (4-methoxy-3-piperazin-1-yl-phenyl)-amide monohydrochloride

参考文献

1. C Routledge, et al. Br J Pharmacol. 2000 Aug;130(7):1606-12.

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