gpr8

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.

Neuropeptide W-23 (human) (NPW-23) TFA, representing the active form of Neuropeptide W, functions as an endogenous agonist for both NPBW1 (GPR7) and NPBW2 (GPR8) receptors [1].

Biotinyl-neuropeptide W-23 (human) is a biotinylated variant of neuropeptide W-23 (human) that acts as an agonist for the NPBW1 (GPR7) and NPBW2 (GPR8) receptors [1] [2].

'(Des-Bromo)-Neuropeptide B (1-23) (human)' is an agonist for orphan G-protein-coupled receptors, exhibiting a K i of 1.2 nM for GPR7 (NPBW1) and 341 nM for GPR8 (NPBW2) respectively [1].

Neuropeptide W-23(human) (NPW-23) is an endogenous ligand for NPBW1 and NPBW2.

Neuropeptide W-30 (human) serves as a crucial stress mediator within the central nervous system, influencing the hypothalamus-pituitary-adrenal (HPA) axis and sympathetic outflow. It acts as an endogenous ligand for the two related orphan G-protein-coupled receptors (GPCRs), GPR7 and GPR8, binding and activating them at comparable effective doses [1] [2] [3].

Neuropeptide W-30 (rat) acts as a crucial stress mediator within the central nervous system, influencing the hypothalamus-pituitary-adrenal (HPA) axis and sympathetic outflow. It serves as an endogenous ligand for the two related orphan G-protein-coupled receptors (GPCRs), GPR7 and GPR8. NPW-30 binds and activates both GPR7 and GPR8 at comparable effective doses [1] [2] [3].