1. Signaling Pathways
  2. GPCR/G Protein
  3. GPR84

GPR84

G protein coupled receptor 84

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.

GPR84 Related Products (12):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-135303
    GLPG1205
    Antagonist 99.64%
    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. GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    GLPG1205
  • HY-12764
    6-OAU
    Agonist 99.91%
    6-OAU (GTPL5846) (6-n-octylaminouracil) is an GPR84 (G protein-coupled receptor 84) agonist, with an EC50 value of 105 nM. 6-OAU works as a chemoattractant to both PMNs and macrophages, and amplifies the proinflammatory cytokine IL-8, shows proinflammatory function. 6-OAU also displays anti-bacterial function.
    6-OAU
  • HY-100775
    Fezagepras sodium
    Antagonist 99.65%
    Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras sodium decreases renal, liver and pancreatic fibrosis. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
    Fezagepras sodium
  • HY-112562
    GPR84 antagonist 8
    Antagonist 99.85%
    GPR84 antagonist 8 is a selective GPR84 antagonist.
    GPR84 antagonist 8
  • HY-124571
    ZQ-16
    Agonist 99.88%
    ZQ-16 is a potent and selective GPR84 agonist with an EC50 value of 0.213 μM. ZQ-16 has no activity on the other free fatty acid receptors (FFARs), including GPR40, GPR41, GPR119 and GPR120.
    ZQ-16
  • HY-161106
    OX04528
    Agonist
    OX04528 (compound 68) is a potent, G-protein biased, and orally active GPR84 agonist. OX04528 no cytotoxicity. OX04528 inhibits cAMP production with an EC50 value of 0.00598 nM.
    OX04528
  • HY-126346
    DL-175
    Agonist
    DL-175 (compound 13) is a selective GPR84 agonist with biased agonistic activity. DL-175 can selectively activate functional responses in immune cells and induce enhanced chemotaxis and phagocytosis of human bone marrow cells. DL-175 is a potential chemical probe.
    DL-175
  • HY-161107
    OX04529
    Agonist
    OX04529 (compound 69) is a potent, selective and orally active agonist of GPR84. OX04529 inhibits FSK-induced cAMP production with an EC50 of 0.0185 nM. OX04529 displayed excellent potency, high G-protein signaling bias.
    OX04529
  • HY-139675
    GPR84 antagonist 1
    Antagonist 99.21%
    GPR84 antagonist 1 is a high affinity and highly selective competitive antagonist of human GPR84.
    GPR84 antagonist 1
  • HY-145697
    GPR84 antagonist 2
    Antagonist 99.53%
    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.
    GPR84 antagonist 2
  • HY-151100
    GPR84 antagonist 3
    Antagonist 99.54%
    GPR84 antagonist 3 (compound 42) is a potent GPR84 (G-protein-coupled receptor 84) antagonist. GPR84 antagonist 3 inhibits GTPγS, with a pIC50 of 8.28. GPR84 antagonist 3 has a favorable pharmacokinetic profile suitable.
    GPR84 antagonist 3
  • HY-100775A
    Fezagepras
    Antagonist
    Fezagepras (Setogepram) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras decreases renal, liver and pancreatic fibrosis. Fezagepras exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
    Fezagepras