2. GPCR/G Protein
  3. GPR84

GPR84

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 (9):

Cat. No. Product Name Effect Purity
  • 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[1]. Fezagepras sodium decreases renal, liver and pancreatic fibrosis[1][2]. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2].
  • HY-139675
    GPR84 antagonist 1 Antagonist 99.21%
    GPR84 antagonist 1 is a high affinity and highly selective competitive antagonist of human GPR84.
  • HY-112562
    GPR84 antagonist 8 Antagonist 99.85%
    GPR84 antagonist 8 is a selective GPR84 antagonist.
  • 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[1][2].
  • 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[1][2].
  • HY-124571
    ZQ-16 Agonist
    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[1].
  • HY-100775A
    Fezagepras Antagonist
    Fezagepras (Setogepram) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[1]. Fezagepras decreases renal, liver and pancreatic fibrosis[1][2]. Fezagepras exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2].
  • 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[1].
  • HY-151100
    GPR84 antagonist 3 Antagonist
    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[1].