Novel small molecule agonist at the CCR8 chemokine receptor (EC50=254nM) with no activity at CCR1, CCR2B, CCR4, CCR5, CXCR2, CXCR3 or CXCR4. Dose dependently increases intracellular calcium and stimulates extracellular acidification in cells expressing human CCR8. Murine CCR8-expressing cells underwent chemotaxis on exposure to this agonist. Inhibits HIV fusion of cells expressing CD4 and CCR8. Small molecule CCR8 agonists represent useful tools for exploring CCR8 biology especially in experiments where the use of the natural protein agonist is impractical.
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Last modified: May 29, 2024
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