g protein coupled receptor 84

Fezagepras (Setogepram) is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84 with anti-inflammatory, anti-fibrotic, and anti-proliferative actions.

6-OAU (GTPL5846)(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

ZQ-16 is a potent and highly selective agonist for the G protein-coupled receptor GPR84, demonstrating a half-maximal effective concentration (EC50) of 0.213 μM, and it activates multiple downstream signaling pathways including calcium mobilization, inhibition of cAMP accumulation, phosphorylation of extracellular signal-regulated protein kinase 1/2 (ERK1/2), receptor desensitization and internalization, and receptor-β-arrestin interaction, making it a useful tool compound for studying GPR84 function and a candidate for further optimization.

GPR84 Antagonist 3 (compound 42), a potent inhibitor of the G-protein-coupled receptor 84 (GPR84), exhibits a pIC50 value of 8.28, indicating strong antagonistic activity by inhibiting GTPγS. Additionally, it possesses a favorable pharmacokinetic profile, suitable for further research and development [1].

PSB-1584 is a Potent Agonist of the Orphan G Protein-Coupled Receptor 84 (GPR84). GPR84, a Gi protein-coupled receptor that is activated by medium-chain (hydroxy)fatty acids, appears to play an important role in inflammation, immunity, and cancer.