1. GPCR/G Protein
  2. Leukotriene Receptor
  3. SB-209247

SB-209247 是一种选择性、高亲和力、具有口服活性的白三烯 B4 (LTB4) 受体拮抗剂,Ki 为 0.78 nM。SB-209247 阻断 LTB4 诱导的 Ca2+ 动员,IC50 为 6.6 nM。SB-209247 显示出有效的抗炎活性。

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SB-209247 Chemical Structure

SB-209247 Chemical Structure

CAS No. : 154413-61-3

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查看 Leukotriene Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a Ki of 0.78 nM. SB-209247 blocks LTB4-induced Ca2+ mobilization with an IC50 of 6.6 nM. SB-209247 shows a potent anti-inflammatory activity[1].

IC50 & Target[1]

LTB4

0.78 nM (Ki)

体外研究
(In Vitro)

SB-209247(化合物 3)表现出对 LTB4 受体的高度选择性。SB-209247 在各自的受体结合测定中与 [3H]-fMLP 和 [3H]LTD4 竞争,IC50 值为 3250 nM 和 16800 nM,并与另外 14 种配体竞争,IC50 值大于 10000 nM。通过阻断 LTB4 诱导的 Ca2+ 动员和 LTB4 诱导的脱颗粒,在人多形核白细胞 (PMN) 中证明了细胞水平的功能活性,IC50 值分别为 6.6 nM 和 53 nM[1]

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

体内研究
(In Vivo)

SB-209247(化合物 3)在小鼠模型中抑制中性粒细胞流入的 ED50 为 14.8 mg/kg,并抑制炎症反应的流体相(水肿),ED50 为 18.7 mg/kg[1]

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

分子量

460.37

Formula

C23H19Cl2NO3S

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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Help & FAQs
  • 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-209247
目录号:
HY-112741
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