GPR

7α,25-Dihydroxycholesterol is a potent agonist of the orphan G protein-coupled receptor GPR183 (EBI2). This compound exhibits high efficacy in activating EBI2, with an EC50 of 140 pM and a Kd of 450 pM. It plays a critical role in chemokine signaling, directing the migration of immune cells such as B cells, T cells, and dendritic cells, making it valuable for research in immunology and cell signaling pathways.

SAE-14 is a selective antagonist of GPR183, exhibiting an IC50 value of 28.5 nM. It effectively inhibits 7α, 25-OHC–induced calcium mobilization in HL-60 cells with an IC50 under 50 nM. SAE-14 has demonstrated potential in reversing allodynia in murine models, making it a valuable tool for research into pain mechanisms and immune regulation.