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. IC50 value: 105 nM Target: GPR84 agonist
CAS Number: 83797-69-7
Molecular Weight: 239.31
Chemical Name: 6-(Octylamino)-2,4(1H,3H)-pyrimidinedione
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: < 7 mg/mL
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
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.
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.
- Suzuki M, et al. Medium-chain fatty acid-sensing receptor, GPR84, is a proinflammatory receptor. J Biol Chem. 2013 Apr 12;288(15):10684-91.
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