2015年4月1日星期三

GTPL 5846|GTPL5846|6-OAU From DC Chemicals

GTPL 5846|GTPL5846|6-OAU From DC Chemicals
DC Chemicals provides GTPL-5846 (6-OAU), other names: GTPL 5846,GTPL5846,6-OAU,GTPL-5846, cas: 83797-69-7. In stock.

Contact: website: www.dcchemicals.com,
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6-OAU(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.

GTPL-5846 (6-OAU), other names: GTPL 5846,GTPL5846,6-OAU,GTPL-5846, cas: 83797-69-7, Molecule formular: C12H21N3O2, Molecule Weight: 239.31, Chemical name:

6-OAU(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.
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 after 6-OAU inoculation.

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