2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Apoptosis
  3. Opioid Receptor Interleukin Related TNF Receptor Sigma Receptor
  4. KOR agonist 7

KOR agonist 7 (Compound 29) 是一种高选择性的 κ-阿片受体 (KOR) 激动剂，其 Ki 为 138 nM。KOR agonist 7 对 μ 和 δ 阿片受体、σ1 受体均无活性，对 σ2 受体 (σ2 receptor) 的亲和力极低 (Ki = 2.8 μM)。KOR agonist 7 能显著降低促炎细胞因子 (如 IL-6、TNF-α、IFN-γ) 的分泌，同时增加抗炎细胞因子 IL-10 的分泌。KOR agonist 7 减少促炎的 M1 型巨噬细胞标志物 (CD80) 的表达，同时增加抗炎的 M2 型巨噬细胞标志物 (CD163) 的表达。KOR agonist 7 可用于镇痛和免疫调节。

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KOR agonist 7

KOR agonist 7 Chemical Structure

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KOR agonist 7 相关抗体

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  • 生物活性

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生物活性

KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a Ki of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (Ki = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation[1].

IC50 & Target[1]

κ Opioid Receptor/KOR

138 nM (Ki)

σ2

2.8 μM (Ki)

IL-6

 

IL-10

 

分子量

411.37

Formula

C21H28Cl2N2O2
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

KOR agonist 7 相关分类

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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.

Keywords:

KOR agonist 7KOR agonist7KOR agonist-7Opioid ReceptorInterleukin RelatedTNF ReceptorSigma ReceptorILTumor Necrosis Factor ReceptorTNFRκ-opioid receptor affinityMorphanEthylenediaminePerillaldehydeChiral pool synthesisCurtius rearrangementSelectivityLigand-lipophilicity efficiency LLEComputational studiesInhibitorinhibitorinhibit

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