GPR84 is a G protein-coupled receptor for medium-chain fatty acids. GPR84 is a receptor for free fatty acids and can be potently activated by saturated medium-chain free fatty acids (MCFAs) like decanoic acid, undecanoic acid and lauric acid. GPR84, a receptor for medium-length free fatty acids is upregulated on protein level in LPS activated tolerant CD14+ monocytes and THP-1 cells. GPR84 is activated by MCFAs with the hydroxyl group at the 2- or 3-position more effectively than nonhydroxylated MCFAs. GPR84 is now considered to be a member of FFA-sensing GPCRs. MCFAs with carbon chain lengths of 9–14 activate GPR84, coupling primarily to a pertussis toxin (PTX)-sensitive Gi/o pathway. GPR84 should be a proinflammatory receptor and may be a novel, attractive target for treating chronic low grade inflammation associated-diseases.


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GPR84 antagonist 2

GPR84 antagonist 2 (compound 33) is a potent, selective, and orally active GPR84 antagonist (IC50=8.95 nM). GPR84 antagonist 2 shows improved potency in the calcium mobilization assay and the ability to inhibit the chemotaxis of neutrophils and macrophages upon GPR84 activation. GPR84 antagonist 2 has the potential for the research of ulcerative colitis[1].

  • CAS Number: 2244269-74-5
  • MF: C28H16Cl2NaO4PS2
  • MW: 605.42
  • Catalog: GPR84
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PBI-4050

Setogepram (PBI-4050) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[1]. Setogepram (PBI-4050) decreases renal, liver and pancreatic fibrosis[1][2]. Setogepram (PBI-4050) exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2].

  • CAS Number: 1002101-19-0
  • MF: C13H18O2
  • MW: 206.28100
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GPR84 antagonist 8

GPR84 antagonist 8 is a selective GPR84 antagonist.

  • CAS Number: 1445846-30-9
  • MF: C23H23N3O5
  • MW: 421.45
  • Catalog: GPR84
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ZQ 16

A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM; does not evoke calcium responses in HEK293 cells expressing other FFARs, including GPR40, GPR41, GPR119, and GPR120; increases in intracellular calcium concentrations in HEK293/Gα16/GPR84 cells with EC50 of 1.01 uM; activates several GPR84-mediated signaling pathways, including calcium mobilization, inhibition of cAMP accumulation, phosphorylation of ERK1/2, receptor desensitization and internalization, and receptor-β-arrestin interaction; reduces forskolin-stimulated cAMP accumulation in HEK293 cells with EC50 of 0.134 uM.

  • CAS Number: 376616-73-8
  • MF: C10H16N2O2S
  • MW: 228.311
  • Catalog: GPR84
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

6-OAU

6-OAU(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.IC50 value: 105 nM [1]Target: GPR84 agonistin vitro: 6-OAU increased [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with an EC50 of 512 nM. 6-OAU did not activate human GPR40 in HEK293 cells in the PI assay. Stimulation with 6.25 μm 6-OAU began to induce GPR84-EGFP internalization, and the extensive internalization was observed at 200 μm 6-OAU stimulation. In a Transwell assay, 3-OH-C12 and the surrogate agonist, 6-OAU, provoked chemotaxis of PMNs prepared from human peripheral blood in a concentration-dependent manner with an EC50 of 24.2 μm and 318 nm, respectively. In addition, 3-OH-C12 and 6-OAU increased the secretion of IL-8 from LPS-stimulated PMNs [1].in vivo: Injection of 6-OAU suspension in 1% rat serum into the rat jugular vein (10 mg/kg) leads to the elevation of a chemokine, CXCL1 concentration in the serum peaking at 3 h after the injection. In the rat air pouch model, 6-OAU at 1 mg/ml dissolved in 0.3% BSA attracted both PMNs and macrophages into the air pouch, peaking at 4 h after 6-OAU inoculation [1].

  • CAS Number: 83797-69-7
  • MF: C12H21N3O2
  • MW: 239.314
  • Catalog: GPR84
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PBI-4050 sodium salt

PBI-4050 acts as an agonist for GPR40 and as an antagonist or inverse agonist for GPR84.

  • CAS Number: 1254472-97-3
  • MF: C13H17NaO2
  • MW: 228.263
  • Catalog: GPR40
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GLPG1205

GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis[1][2].

  • CAS Number: 1445847-37-9
  • MF: C22H22N2O4
  • MW: 378.42
  • Catalog: GPR84
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A