gpr-183

SAE-14 is a specific GPR183 antagonist. SAE-14 inhibits GPR183 with an IC50 of 28.5 nM in a calcium mobilization assay[1].

7α,25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist, as well as an endogenous ligand, of the orphan GPCR receptor EBI2 (GPR183). It serves as a chemokine directing the migration of B cells, T cells, and dendritic cells and exhibits high potency in activating EBI2 (EC50=140 pM; Kd=450 pM) [1][2].

NIBR189 is a potent and selective antagonist of EBI2 (GPR183) receptor (IC50 of 11 and 15 nM for human and mouse EBI2 receptors, respectively)

ML401 is a selectively EBI2(GPR183) receptor antagonist(IC50 of 1.03 nM) .

GPR183 antagonist-3 (compound 33) is an orally active GPR183 antagonist with an IC50 value of 8.7 μM. It demonstrates significant in vitro anti-migration and anti-inflammatory activity in monocytes and can alleviate pathological symptoms in experimental colitis induced by dextran sulfate sodium.

GPR183 inverse agonist-1 (Compound 78) is an inverse agonist of GPR183. It inhibits GPR183-mediated Gi activation and β-arrestin2 recruitment while blocking PBMC migration. This compound is utilized in research concerning inflammation, autoimmune, and cancer-related diseases.

GSK682753A is a selective and highly potent inverse agonist of the Epstein-Barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.