1. GPCR/G Protein Stem Cell/Wnt MAPK/ERK Pathway Anti-infection
  2. GPR84 ERK Bacterial Antibiotic
  3. 6-OAU

6-OAU (GTPL5846) (6-n-octylaminouracil) is an GPR84 (G protein-coupled receptor 84) agonist, with an EC50 value of 105 nM. 6-OAU works as a chemoattractant to both PMNs and macrophages, and amplifies the proinflammatory cytokine IL-8, shows proinflammatory function. 6-OAU also displays anti-bacterial function.

For research use only. We do not sell to patients.

6-OAU Chemical Structure

6-OAU Chemical Structure

CAS No. : 83797-69-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 526 In-stock
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10 mM * 1 mL in DMSO USD 526 In-stock
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5 mg USD 420 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE 6-OAU

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

6-OAU (GTPL5846) (6-n-octylaminouracil) is an GPR84 (G protein-coupled receptor 84) agonist, with an EC50 value of 105 nM. 6-OAU works as a chemoattractant to both PMNs and macrophages, and amplifies the proinflammatory cytokine IL-8, shows proinflammatory function. 6-OAU also displays anti-bacterial function[1][2].

IC50 & Target

ERK

 

Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.0167 μM
Compound: 3
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay
[PMID: 31721581]
CHO EC50
0.114 μM
Compound: 3
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
[PMID: 31721581]
HEK293 EC50
0.105 μM
Compound: 3
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method
Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method
[PMID: 31721581]
HEK293 EC50
0.341 μM
Compound: 3
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF as
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF as
[PMID: 31721581]
HEK293 EC50
0.653 μM
Compound: 6-OAU
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
[PMID: 27326330]
HEK293 EC50
1.25 μM
Compound: 3
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
[PMID: 31721581]
HEK293 EC50
1.75 μM
Compound: 3
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
[PMID: 31721581]
HEK293 EC50
438 nM
Compound: 6-OAU
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
[PMID: 27326330]
Sf9 EC50
0.512 μM
Compound: 3
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting method
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting method
[PMID: 31721581]
Sf9 EC50
512 nM
Compound: 6-OAU
Agonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
Agonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
[PMID: 27326330]
In Vitro

GPR84 gene exhibits high expression in human polymorphonuclear leukocytes (PMNs) and macrophages, 6-OAU acts on proinflammatory function by activitating GPR84[1].
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[1].
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[1].
6-OAU (1 nM-1 mM; 1 h) provokes chemotaxis of PMNs in a concentration-dependent manner with an EC50 value of 318 nM[1].
6-OAU (0-10 μM; 4 h) increases the secretion of IL-8 from LPS-stimulated PMNs[1].
6-OAU (0-0.4 μM; 16 h) also amplifies TNF-α production from U937 macrophages[1].
6-OAU (2 μM; 4 h) decreases ERK phosphorylation and MCP-1 protein expression, (2 μM; 48 h) decreases MCP-1 secretion in macrophages [2].
6-OAU (2 μM; 24 h) reduces ROS production during B. abortus infection in RAW264.7 cells[2].
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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

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[2]

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.
In Vivo

6-OAU activates GPR84 and results in making an inflammatory condition through chemokine production and chemotaxis in vivo[1].
6-OAU (10 mg/kg; i.v.) raises the blood CXCL1 level in rats[1].
6-OAU (1 mg/mL; s.c.) attracts both PMNs and macrophages into the air pouch[1].
6-OAU (2 μM, 100 mL/mouse; s.c.) augments resistance to Brucella infection, and reduces bacterial proliferation in spleens and livers[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Lewis rats(4-week-old)[1]
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)[1]
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)[2]
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.
Lowed splenic weight of mice and splenic proliferation.
Molecular Weight

239.31

Formula

C12H21N3O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NC(C=C(NCCCCCCCC)N1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (104.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1787 mL 20.8934 mL 41.7868 mL
5 mM 0.8357 mL 4.1787 mL 8.3574 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.91%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.1787 mL 20.8934 mL 41.7868 mL 104.4670 mL
5 mM 0.8357 mL 4.1787 mL 8.3574 mL 20.8934 mL
10 mM 0.4179 mL 2.0893 mL 4.1787 mL 10.4467 mL
15 mM 0.2786 mL 1.3929 mL 2.7858 mL 6.9645 mL
20 mM 0.2089 mL 1.0447 mL 2.0893 mL 5.2234 mL
25 mM 0.1671 mL 0.8357 mL 1.6715 mL 4.1787 mL
30 mM 0.1393 mL 0.6964 mL 1.3929 mL 3.4822 mL
40 mM 0.1045 mL 0.5223 mL 1.0447 mL 2.6117 mL
50 mM 0.0836 mL 0.4179 mL 0.8357 mL 2.0893 mL
60 mM 0.0696 mL 0.3482 mL 0.6964 mL 1.7411 mL
80 mM 0.0522 mL 0.2612 mL 0.5223 mL 1.3058 mL
100 mM 0.0418 mL 0.2089 mL 0.4179 mL 1.0447 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
6-OAU
Cat. No.:
HY-12764
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