J 113863

Uses

cis-J-113863 is a competitive chemokine receptor 1 (CCR1) antagonist, with IC50 values of 0.9 and 5.8 nM for human and mouse CCR1 receptors, respectively[1].

Biological Activity

J113863 is a high affinity antagonist for CCR1 and CCR3 receptors. Also both J113863 and its enantiomer c exhibit low binding affinity toward CCR2 and CCR5 where they activate three Gi and two G0 protein isoforms. J113863 does not activate G12 protein isoform. J113863 binding to CCR2 and CCR5 induce the recruitment of b-arrestin 2 whereas UCB35625 did not. J113863 and UCB35625 are biased ligands for the chemokine receptors CCR2 and CCR5.

References

[1] M Amat, et al. Pharmacological blockade of CCR1 ameliorates murine arthritis and alters cytokine networks in vivo. Br J Pharmacol. 2006 Nov;149(6):666-75. DOI:10.1038/sj.bjp.0706912

Raw materials

Preparation Products