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Ketotifen fumarate (HC 20511 fumarate) is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators.

JNJ4796 is an orally active fusion inhibitor of the influenza virus, inhibiting hemagglutinin (HA)-mediated fusion to neutralize the influenza A group 1 virus. JNJ4796 mimics the functionality of broadly neutralizing antibodies (bnAbs).

GPR84 antagonist 8 is a selective GPR84 antagonist applicable for investigating inflammatory and fibrotic diseases.

GPR84agonist-2 (Compound 8e) is a highly selective GPR84 agonist with an EC50 value of 7.24 nM. It activates the Gαq signaling pathway, leading to the production of inositol triphosphate (IP3) and the release of calcium ions. This compound enhances the chemotaxis of neutrophils and the release of pro-inflammatory cytokines, making it a promising candidate for research into inflammatory diseases such as ulcerative colitis and acute lung injury.

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

GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.

GPR84 Antagonist 3 (compound 42), a potent inhibitor of the G-protein-coupled receptor 84 (GPR84), exhibits a pIC50 value of 8.28, indicating strong antagonistic activity by inhibiting GTPγS. Additionally, it possesses a favorable pharmacokinetic profile, suitable for further research and development [1].

GPR84 Antagonist 2, a potent and selective GPR84 antagonist (IC 50 = 8.95 nM), demonstrates oral activity and significantly enhances potency in calcium mobilization assays. It effectively inhibits neutrophil and macrophage chemotaxis following GPR84 activation, highlighting its research potential for ulcerative colitis.

GPR81 agonist 2 is a potent agonist targeting the GPR81 receptor, demonstrating EC50 values of 0.023 µM for hGPR81 and 0.123 µM for hGPR109A, respectively.

GPR88-IN-1 is a GPR88 antagonist that can be used for researching central nervous system disorders [1].

GPR88 agonist 2 (compound 53) is a potent, brain-penetrant agonist of GPR88, with an EC50 of 14 µM in the GPR88 cAMP functional assay [1].

GPR88 agonist 3 (compound 20), exhibiting an EC50 of 204 nM, functions as an agonist for GPR88. It is applicable in the research of psychiatric and neurodegenerative disorders [1].

GPR84antagonist 9 is an orally active GPR84 antagonist with an IC50 value of 0.012 μM. It can be utilized in research on inflammatory pain diseases.

GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and can be used to study pulmonary fibrosis.

(1R,2R)-2-PCCA hydrochloride is a potent, selective, and blood-brain-barrier-crossing GPR88 receptor agonist with an EC50 value of 1140 n in striatal membranes of WT mice; it can be used to study the central nervous system.

Lactic acid (2-hydroxypropanoic acid), a glycolysis end product, is a hydroxycarboxylic acid receptor 1 (HCAR1) activator (EC50=4.2-5 mM). Lactic acid can be used as a hemodynamic index in critically ill patients and has anti-tumor activity.

IPR-803 is an effective inhibitor of the uPAR·uPA protein-protein interaction (PPI) with anti-tumor activity. IPR-803 binds directly to uPAR with a Ki of 0.2 μM.

RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, exhibiting an EC50 of 25 nM in vitro cAMP functional assay. It significantly reduces alcohol reinforcement and intake behaviors in rats [1].

RTI-13951-33 is an effective and brain-penetrant GPR88 agonist (EC50: 25 nM, in GPR88 cAMP functional assay).

Fezagepras (Setogepram) is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84 with anti-inflammatory, anti-fibrotic, and anti-proliferative actions.

6-OAU (GTPL5846)(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.

PR825 is a β5c inhibitor with IC50 = 20 nM

3-chloro-5-hydroxy Benzoic Acid (3-chloro-5-hydroxy BA) is an agonist of GPR81 (EC50 : 16 μM)

OX04528 is an orally active and potent GPR84 biased agonist.OX04528 inhibits cAMP signaling and may be useful in cancer research.