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| Targets |
hGPR84 ( EC50 = 105 nM ); human GPR84-Gαi fusion protein ( EC50 = 512 nM )
GPR84 (G protein-coupled receptor 84), a receptor activated by medium-chain fatty acids. As an agonist, GTPL5846 binds to and activates GPR84, leading to downstream signaling via G proteins. |
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| ln Vitro |
Human macrophages and polymorphonuclear leukocytes (PMNs) have high expression levels of the GPR84 gene, and 6-OAU activates GPR84 to promote proinflammatory activity[1].
6-OAU (0.01 nM-0.1 mM; 1 h) with an EC50 value of 105 nM in HEK293 cells activates human GPR84[1].
6-OAU (0, 6.25, 200 μM; 30 min) incites GPR84-EGFP internalization in a GPR84-dependent manner, accumulates phosphoinositides, and stimulates [35S]GTP binding[1]. 6-OAU (1 nM-1 mM; 1 h) has an EC50 value of 318 nM and causes PMN chemotaxis in a concentration-dependent manner[1]. 6-OAU (0–10 μM; 4 h) stimulates LPS-stimulated PMNs to secrete more IL-8[1]. 6-OAU (0-0.4 μM; 16 h) also increases U937 macrophages' production of TNF-α[1]. 6-OAU (2 μM; 4 h) inhibits MCP-1 protein expression and ERK phosphorylation, and (2 μM; 48 h) inhibits MCP-1 secretion in macrophages[2]. 6-OAU (2 μM; 24 h) decreases ROS generation in RAW264.7 cells infected with B. abortus[2]. 6-OAU (2 μM; 0, 30, and 60 min) suppresses adhesion and anti-Bryella and anti-Salmonella activity in RAW264.7 cells, and (2 μM; 30 min) exhibits anti-infection against both infections[2]. In HEK293 cells expressing human GPR84 with Gqi5 chimera, GTPL5846 activates the receptor with an EC50 of 105 nM in the PI (phosphatidylinositol) assay. It has a chemotactic effect on neutrophils and macrophages and amplifies IL-8 production. These activities confirm its role as a GPR84 agonist with pro-inflammatory properties. |
| ln Vivo |
6-OAU triggers the production of chemokines and chemotaxis in vivo, which in turn activates GPR84 and causes an inflammatory state[1].
6-OAU (10 mg/kg; i.v.) increases the level of CXCL1 in the blood in rats[1]. 6-OAU (1 mg/mL; s.c.) draws macrophages and PMNs into the air pouch[1]. 6-OAU (2 μM, 100 mL/mouse; s.c.) decreases bacterial growth in the liver and spleen and increases resistance to Brucella infection[2]. Specific in vivo activity data for GTPL5846 are not detailed in the available literature. As a GPR84 agonist, it would be expected to modulate inflammatory responses in vivo, but specific animal model studies are not described. |
| Enzyme Assay |
The in vitro assay for GTPL5846 involves measuring GPR84 activation in a cellular system. HEK293 cells are engineered to express human GPR84 along with a Gqi5 chimera, which couples the receptor to the phospholipase C pathway. Cells are loaded with a fluorescent calcium indicator or a PI assay is used. GTPL5846 is added at various concentrations, and the calcium flux or PI hydrolysis is measured. The EC50 is determined from the dose-response curve.
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| Cell 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. The in vitro cell-based assay for GTPL5846 is the same as described above. HEK293 cells expressing GPR84 and Gqi5 are used. This is a functional cell-based assay that measures receptor activation in a living cell. The assay can be adapted to measure other downstream effects, such as chemotaxis or cytokine production in immune cells. |
| Animal Protocol |
Female Lewis rats(4-week-old)
10 mg/kg Intravenous injection; collecting blood 3 h after injection Specific in vivo animal model protocols for GTPL5846 are not described. To evaluate its in vivo activity, GTPL5846 could be administered to animal models of inflammation. Endpoints would include measurement of inflammatory markers, immune cell infiltration, and tissue pathology. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for GTPL5846 are not reported in the available literature. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties have not been extensively characterized. Studies would be needed to determine its bioavailability, half-life, and tissue distribution.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GTPL5846 are not available. As a research compound, its safety profile has not been comprehensively characterized. Toxicity studies would be required to determine its safety margin and potential off-target effects.
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| References |
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| Additional Infomation |
GTPL5846 is primarily a research tool for studying GPR84 function and its role in inflammation and immune responses. It is used to investigate the signaling pathways activated by GPR84 and to explore the potential of GPR84 as a therapeutic target for inflammatory diseases. It is not an approved therapeutic agent.
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| Molecular Formula |
C12H21N3O2
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| Molecular Weight |
239.319
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| Exact Mass |
239.163
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| Elemental Analysis |
C, 60.23; H, 8.85; N, 17.56; O, 13.37
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| CAS # |
83797-69-7
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| PubChem CID |
10354234
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Index of Refraction |
1.520
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| LogP |
2.77
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
17
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| Complexity |
300
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1NC(=O)NC(NCCCCCCCC)=C1
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| InChi Key |
PFSWASUQURIOOR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H21N3O2/c1-2-3-4-5-6-7-8-13-10-9-11(16)15-12(17)14-10/h9H,2-8H2,1H3,(H3,13,14,15,16,17)
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| Chemical Name |
6-(octylamino)-1H-pyrimidine-2,4-dione
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| Synonyms |
GTPL-5846; GTPL 5846; GTPL5846
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25~35 mg/mL (104.5~146.3 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1785 mL | 20.8925 mL | 41.7851 mL | |
| 5 mM | 0.8357 mL | 4.1785 mL | 8.3570 mL | |
| 10 mM | 0.4179 mL | 2.0893 mL | 4.1785 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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