GTPL5846

Description	in vitro: 6-OAU increased [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with an EC50 of 512 nM. 6-OAU did not activate human GPR40 in HEK293 cells in the PI assay. Stimulation with 6.25 μm 6-OAU began to induce GPR84-EGFP internalization, and the extensive internalization was observed at 200 μm 6-OAU stimulation. In a Transwell assay, 3-OH-C12 and the surrogate agonist, 6-OAU, provoked chemotaxis of PMNs prepared from human peripheral blood in a concentration-dependent manner with an EC50 of 24.2 μm and 318 nm, respectively. In addition, 3-OH-C12 and 6-OAU increased the secretion of IL-8 from LPS-stimulated PMNs. in vivo: Injection of 6-OAU suspension in 1% rat serum into the rat jugular vein (10 mg/kg) leads to the elevation of a chemokine, CXCL1 concentration in the serum peaking at 3 h after the injection. In the rat air pouch model, 6-OAU at 1 mg/ml dissolved in 0.3% BSA attracted both PMNs and macrophages into the air pouch, peaking at 4 h
Pathways	Hormone Pathay GPCR/G Protein
Targets	GPR

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