KOR agonist 7
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].
Product Specifications
UNSPSC
12352005
Target
Interleukin Related; Opioid Receptor; Sigma Receptor; TNF Receptor
Related Pathways
Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling
Field of Research
Inflammation/Immunology; Neurological Disease
Smiles
O[C@](CN1C(CC2=CC=C(Cl)C(Cl)=C2)=O)(C)[C@H]3CC[C@@H](N4CCCC4)[C@@H]1C3
Molecular Formula
C21H28Cl2N2O2
Molecular Weight
411.37
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
IL-10; IL-6; Sigma 2 Receptor; κ Opioid Receptor/KOR
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