R243

R243 is a potent, small molecule CCR8 antagonist that inhibits CCR8 signaling and chemotaxis, inhibits CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation at 0.2 uM; attenuated secretion of TNF-α, IL-6, and most strikingly IL-10 from WT PMφ (peritoneal macrophages), but not BMMφ (bone marrow-derived macrophages); shows suppressed c-JNK activity and NF-κB signaling after LPS treatment, suppresses LPS-induced cytokine secretion; attenuates peritoneal adhesions in vivo in CCR8-/- mice, also prevents hapten-induced colitis.

References 1. Oshio T, et al. PLoS One. 2014 Apr 8;9(4):e94445. 2. Berenguer J, et al. J Extracell Vesicles. 2018 Mar 13;7(1):1446660. View Related Products by Target Chemokine Receptor (CCR and CXCR)