gpr183

GPR183-IN-1 (compound 15) is an effective orally active inhibitor of GPR183. It inhibits Ca2+ mobilization with an IC50 value of 39.97 nM. GPR183-IN-1 holds potential for research in cancer, autoimmune diseases, pain, and osteoporosis.

GPR183-IN-2 (compound 23) is an effective, orally active inhibitor of GPR183, displaying an IC50 value of 39.45 nM in Ca2+ mobilization assays. This compound has potential applications in research related to cancer, autoimmune diseases, pain, and osteoporosis.

GPR183 antagonist-2 (compound 32), a selective antagonist of GPR183, exhibits excellent water solubility and pharmacokinetic properties. This compound effectively diminishes paw and joint swelling, and reduces gene expression of pro-inflammatory cytokines (MCP-1, MMPs, and VEGF) in a dose-dependent manner within a collagen-induced arthritis (CIA) mouse model. GPR183 antagonist-2 is applicable in researching autoimmune diseases [1].

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

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].

PSB-KK1445 is a potent and selective agonist of GPR18, exhibiting EC50 values of 45.4 nM for humans and 124 nM for mice. The selectivity of PSB-KK1445 for GPR18 over the CB receptor subtypes GPR55 and GPR183 exceeds 200-fold.

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.

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