Chemical Name:2-[2-[4-[(3-phenoxyphenyl)methyl]-1-piperazinyl]ethoxy]
ethanol dihydrochloride
Biological Activity:
Selective,
non-peptide CCR8 chemokine receptor agonist (IC50 values are 1.8 and
2.6 μM for human and mouse receptors respectively). Displays no
activity at CCR4, CXCR3, CXCR4 and CCR5 and shows > 28-fold selectivity over
26 other GPCRs (less selective at α2A and 5-HT receptors). Induces
chemotaxis and inhibits Env-mediated (HIV) cell-cell fusion.
Haskellet al (2006) Identification
and characterization of a potent, selective nonpeptide agonist of the CC
chemokine receptor CCR8. Mol.Pharmacol. 69 309.
Potent and selective CXCR2 chemokine receptor antagonist (IC50 = 22 nM) that displays > 150-fold selectivity over CXCR1 receptors. Causes inhibition of IL-8 and GROα-mediated calcium mobilisation in HL60 cells (IC50 values are 8 and 10 nM respectively).
