pr8

GPR84 antagonist 8 is a selective GPR84 antagonist.

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.

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).

Prednisone 21-aldehyde is a derivative of the synthetic corticosteroid prednisone that has antiviral activity against influenza virus A-PR8 in embryonated chicken eggs. 22-hydroxy Prednisone is an unstable adduct of prednisone. It has been observed following incubation of prednisone with nornicotine. This product is a mixture of prednisone 21-aldehyde and 22-hydroxy prednisone.

CAY10766 is an antiviral compound.1It inhibits entry of influenza virus-like particles pseudotyped with hemagglutinin A (HA) from H5N1 influenza A virus into A549 cells (EC50= 0.24 μM). CAY10766 (1 μM) reduces H1N1 and H5N1 influenza A viral titers in infected MDCK cells. It also exhibits synergy with oseltamivir carboxylate in MDCK cells infected with the influenza A reporter PR8-NS1-Gluc virus.

Urumin, a compound with antiviral properties, inhibits human influenza A virus growth, particularly the PR8 strain, with an inhibitory concentration (IC 50) of 3.8 μM. It acts by targeting the conserved stalk of H1 hemagglutinin and can neutralize drug-resistant H1 influenza viruses. Additionally, Urumin offers protective effects against lethal influenza infection in naive mice [1].

Antiviral agent 43 (compound 16) serves as a potent, orally active inhibitor of influenza A virus entry, demonstrating efficacy by inhibiting the replication of the influenza A strains VH04-H5N1 and PR8-H1N1 with EC50 values of 240 nM and 72 nM, respectively [1].