GPR84 Antagonist

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.

GPR84 antagonist 8 is a selective GPR84 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 (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.

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

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.

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.

Fezagepras (sodium) (Standard) is the analytical standard of Fezagepras (sodium). This product is intended for research and analytical applications. 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.

GPR84 antagonist 11 is a highly selective GPR84 antagonist, with a human pA₂ of 8.41 and a pK_i of 8.16. GPR84 antagonist 11 competitively inhibits the binding of agonists to the orthosteric site of GPR84 and has improved druglike properties, though its metabolic stability still requires optimization. GPR84 antagonist 11 can be used in the research of autoimmune diseases and fibrotic diseases.

Fezagepras (Standard) is the analytical standard of Fezagepras. This product is intended for research and analytical applications. 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.