1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. SB 271046

SB 271046 是一种有效的、选择性的、具有口服活性的 5-HT6 受体拮抗剂,pKi 为 8.92-9.09。SB 271046 对 5-HT6 受体的选择性比其他受体、结合位点和离子通道高 200 倍以上。SB 271046 具有抗惊厥活性。

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SB 271046 Chemical Structure

SB 271046 Chemical Structure

CAS No. : 209481-20-9

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SB 271046 的其他形式现货产品:

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Other Forms of SB 271046:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pKi of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity[1].

IC50 & Target[1]

5-HT6 Receptor

8.92-9.09 (pKi)

体外研究
(In Vitro)

In functional studies on human 5-HT6 receptors SB 271046 competitively antagonized 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SB 271046 produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ⩽0.1 mg/kg p.o. and maximum effect at 4 h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB 271046 (EC50 of 0.16 μM) and brain concentrations of 0.01-0.04 μM at Cmax[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

451.99

Formula

C20H22ClN3O3S2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
SB 271046
目录号:
HY-14336
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