GTPL5846

SKU: orb1223903

Description

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.

Images & Validation

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Key Properties

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CAS Number	83797-69-7
MW	239.31
Purity	>98% (HPLC)
Formula	C₁₂H₂₁N₃O₂
SMILES	O=C1NC(C=C(NCCCCCCCC)N1)=O
Target	GPR
Solubility	DMSO: 10 mM

Bioactivity

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In Vivo

6-OAU activates GPR84 and results in making an inflammatory condition through chemokine production and chemotaxis In vivo. 6-OAU (10 mg/kg; i. v.) raises the blood CXCL1 level in rats. 6-OAU (1 mg/mL; s. c.) attracts both PMNs and macrophages into the air pouch. 6-OAU (2 μM, 100 mL/mouse; s. c.) augments resistance to Brucella infection, and reduces bacterial proliferation in spleens and livers. Animal model: Female Lewis rats(4-week-old). Dosage: 10 mg/kg. Administration: Intravenous injection; collecting blood 3 h after injection. Result: Increased the elevation of a chemokine, CXCL1 concentration in the serum peaking at 3 h after the injection. Animal model: Rat air pouch model (4-week-old female rats). Dosage: 1 mg/mL (PBS). Administration: Subcutaneous injection; washing the cavity 4 h after injection. Result: Attracted both PMNs and macrophages into the air pouch, peaking at 4 h after the injection. Animal model: ICR female mice (7-week-old). Dosage: 2 μM (100 μL/mouse). Administration: Oral average; 7 days and another 14 days after treated mouse with B. abortus (2 × 105 CFU /100 μL; i.p.). Result: Reduced bacterial proliferation in the liver and spleen, and decreased IFN-γ but augmented IL-6 serum level.

In Vitro

GPR84 gene exhibits high expression in human polymorphonuclear leukocytes (PMNs) and macrophages, 6-OAU acts on proinflammatory function by activitating GPR84.6-OAU (0.01 nM-0.1 mM; 1 h) activates human GPR84 in the presence of Gqi5 chimera with an EC50 value of 105 nM in HEK293 cells.6-OAU (0, 6.25, 200 μM; 30 min) stimulates [35S]GTP binding, accumulates phosphoinositides, and induces GPR84-EGFP internalization in a GPR84-dependent manner.6-OAU (1 nM-1 mM; 1 h) provokes chemotaxis of PMNs in a concentration-dependent manner with an EC50 value of 318 nM.6-OAU (0-10 μM; 4 h) increases the secretion of IL-8 from LPS-stimulated PMNs.6-OAU (0-0.4 μM; 16 h) also amplifies TNF-α production from U937 macrophages.6-OAU (2 μM; 4 h) decreases ERK phosphorylation and MCP-1 protein expression, (2 μM; 48 h) decreases MCP-1 secretion in macrophages.6-OAU (2 μM; 24 h) reduces ROS production during B. abortus infection in RAW264.7 cells.6-OAU (2 μM; 0, 30, and 60 min) inhibits adhesion and Brucella uptake in RAW264.7 cells and (2 μM; 30 min) shows anti-infection against Brucella and Salmonella infection. Cell Viability Assay Cell line: B. abortus Concentration: 0, 0.02, 0.2, 2 μM Incubation time: 0, 2, 24, 48, 72 hours. Result: Decreased B. abortus survivability begin at 48 h with a dose of 2 μM. Western blot analysis. Cell line: RAW264.7 cells infected with B. abortus Concentration: 2 μM. Incubation time: 4 hours. Result: Reduced ERK phosphorylation and MALT1 expression in RAW264.7 macrophages.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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GTPL5846 | GTPL 5846 | GTPL-5846.

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GPR

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GTPL5846 (orb1223903)

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Purity:	99.68%
CAS Number:	83797-69-7
MW:	239.31
Formula:	C₁₂H₂₁N₃O₂

GTPL5846

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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6-OAU [orb1306678]

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GTPL5846 (orb1223903)

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