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  3. GPCR/G Protein
  4. GPR84

GPR84

G protein coupled receptor 84

GPR84

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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 Produits associés (29):

Cat. No. Nom du produit Effet Pureté Chemical Structure
  • HY-135303
    GLPG1205
    		Antagonist 99.94%
    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 99.77%
    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-112562
    GPR84 antagonist 8
    		Antagonist 99.93%
    GPR84 antagonist 8 is a selective GPR84 antagonist.
    GPR84 antagonist 8
  • HY-100775
    Fezagepras sodium
    		Antagonist 99.78%
    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-100775A
    Fezagepras
    		Antagonist 99.38%
    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
  • HY-180488
    GPR84 antagonist 10
    		Antagonist
    GPR84 antagonist 10 (compound 1) is a potent and orally active GPR84 antagonist. GPR84 antagonist 10 can be used to study GPR84-dependent diseases, such as inflammation-driven pain diseases.
    GPR84 antagonist 10
  • HY-182723
    PSB-16671
    		Activator
    PSB-16671 is an allosteric agonist of GPR84. PSB-16671 recruits β-arrestins and couples to Gi, enhances the Gi activation potency of orthosteric agonists, and exerts a synergistic effect with orthosteric agonists. PSB-16671 promotes G protein activation and partial chemotaxis independent of GPR84 in mouse neutrophils, maintains the phagocytic function of macrophages against cancer cells without inducing receptor desensitization. PSB-16671 can be used in cancer-related research.
    PSB-16671
  • HY-179471
    PSB-17365
    		Agonist
    PSB-17365 is a potent GPR84 agonist with EC50 values of 2.5 nM and 100 nM in a cAMP accumulation assay and a β-arrestin 2 recruitment assay, respectively.
    PSB-17365
  • HY-151100
    GPR84 antagonist 3
    		Antagonist 98.32%
    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-124571
    ZQ-16
    		Agonist 99.0%
    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 98.45%
    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-145697
    GPR84 antagonist 2
    		Antagonist 99.06%
    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-163350
    TUG-2208
    		Agonist 98.09%
    TUG-2208 (compound 42a) is a GPR84 agonist (pEC50=8.98) with low lipophilicity and good solubility, in vitro permeability and microsomal stability.
    TUG-2208
  • HY-126346
    DL-175
    		Agonist 99.0%
    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-178234
    LY237
    		Agonist 99.96%
    LY237 is a highly efficient complete agonist of GPR84 (pEC50 = 10.15). LY237 can be used for research on inflammation and fibrosis conditions.
    LY237
  • HY-139675
    GPR84 antagonist 1
    		Antagonist 98.56%
    GPR84 antagonist 1 is a high affinity and highly selective competitive antagonist of human GPR84.
    GPR84 antagonist 1
  • HY-171115
    Pyrone-211
    		Agonist 99.32%
    Pyrone-211 is a potent GPR84 agonist and AKR1C3 inhibitor. Pyrone-211 participates in an expanded polyamine pathway.
    Pyrone-211
  • HY-173556
    GPR84 agonist-2
    		Agonist 99.80%
    GPR84 agonist-2 is a selective GPR84 agonist with no activity at free fatty acid receptors. GPR84 agonist-2 enhances GPR84-mediated signaling above basal levels and potentiates agonist-induced GPR84 activation. GPR84 agonist‑2 can be used for research on GPR84-related physiological mechanisms.
    GPR84 agonist-2
  • HY-176039
    TUG-2181
    		Antagonist 98.20%
    TUG-2181 is an antagonist of GPR84 with an IC50 value of 34 nM. TUG-2181 inhibits GPR84 agonists-induced reactive species oxygen (ROS) production and IL-8 release in human neutrophils. TUG-2181 can be used for inflammation and fibrosis study.
    TUG-2181
  • HY-161682
    GPR84 antagonist 9
    		Antagonist
    GPR84 antagonist 9 (compound 320) is an orally active GPR84 antagonist with the IC50 of 0.012 μM. GPR84 antagonist 9 can be used for study of inflammatory-driven pain diseases.
    GPR84 antagonist 9