gpr84

GPR84 antagonist 8 is a selective GPR84 antagonist applicable for investigating inflammatory and fibrotic diseases.

GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and can be used to study pulmonary fibrosis.

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.

OX04528 is an orally active and potent GPR84 biased agonist.OX04528 inhibits cAMP signaling and may be useful in cancer research.

GPR84agonist-2 (Compound 8e) is a highly selective GPR84 agonist with an EC50 value of 7.24 nM. It activates the Gαq signaling pathway, leading to the production of inositol triphosphate (IP3) and the release of calcium ions. This compound enhances the chemotaxis of neutrophils and the release of pro-inflammatory cytokines, making it a promising candidate for research into inflammatory diseases such as ulcerative colitis and acute lung injury.

GPR84 antagonist 1 is a highly selective, high-affinity competitive antagonist of human GPR84.

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].

GPR84 Antagonist 2, a potent and selective GPR84 antagonist (IC 50 = 8.95 nM), demonstrates oral activity and significantly enhances potency in calcium mobilization assays. It effectively inhibits neutrophil and macrophage chemotaxis following GPR84 activation, highlighting its research potential for ulcerative colitis.

GPR84antagonist 9 is an orally active GPR84 antagonist with an IC50 value of 0.012 μM. It can be utilized in research on inflammatory pain diseases.

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

2-(pentylsulfanyl)pyrimidine-4,6-diol is a novel GRP84 agonist.

LY-237 is a GPR84 agonist with a cAMP EC50 value of 0.352 nM.

Pyrone-211 acts as a potent GPR84 agonist and an AKR1C3 inhibitor. It is involved in the extended polyamine pathway.

TUG-2181 is an antagonist of GPR84, with an IC50 value of 34 nM. It inhibits reactive oxygen species (ROS) production and IL-8 secretion induced by GPR84 agonists in human neutrophils. TUG-2181 is applicable for research in inflammation and fibrosis.

OX04529 (compound 69) is a potent and orally active GPR84 selective agonist. It inhibits FSK-induced cAMP production with an EC50 of 0.0185 nM and demonstrates exceptional potency along with significant bias towards G protein signaling pathways.

TUG-2099 (compound 4s) is a potent GPR84 agonist with an EC50 of 0.3 nM. It is applicable for research in Alzheimer's disease, atherosclerosis, cancer, and other conditions.

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.

Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bone marrow-derived macrophages (BMDMs) in a cellular impedance assay, and promotes phagocytosis by M1 polarized U937 cells. Induces migration of primary human monocytes, but has no effect on macrophage chemotaxis.

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.

PSB-17365 is a potent GPR84 agonist. PSB-17365 exhibits EC50 values vs. GPR84 of 2.5nM in a cAMP accumulation assay, and 100nM in a β-arrestin 2 recruitment assay. No direct binding affinities are provided. PSB-17365 is selective for GPR84 compared to other free fatty acid receptors (FFAR1 and FFAR4). 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.

PSB-15160 is a compound that inhibits the growth of MCF7 (breast), NCI-H460 (lung) and SF-268 (NCS) cells in the treatment of estrogen-dependent tumours.