| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
GlyT2 5.1 μM (IC50)
GPR18. N-Arachidonylglycine is a full agonist at GPR18 with an EC50 of 44.5 nM. |
|---|---|
| ln Vitro |
In GPR18-transfected HEK293 cells, N-arachidonylglycine (0.1 nM-100 µM; 5 min) induces MAPK activation[1]. Even at doses up to 100 μm, N-arachidonylglycine exhibits no action at GLYT1 or GAT1[2].
N-Arachidonylglycine is a full agonist at GPR18 with an EC50 of 44.5 nM. It is an endogenous anti-inflammatory lipoamino acid. Unlike anandamide, NA-Gly does not activate cannabinoid receptors CB1 and CB2, making it a selective tool for studying GPR18-mediated signaling. |
| ln Vivo |
Anandamide blood concentrations are increased nine times by oral N-arachidonylglycine (10 mg/kg)[3]. The oral administration of N-arachidonylglycine (1.2 mg/kg; once) significantly reduces peritoneal cells by 70%[3].
In vivo, N-arachidonylglycine has been shown to have anti-inflammatory properties. As a GPR18 agonist, it modulates immune responses and inflammation. |
| Enzyme Assay |
In vitro receptor binding assays for N-arachidonylglycine are performed to evaluate its affinity for GPR18. Radioligand binding studies using membrane preparations from cells expressing GPR18 are conducted. The compound's ability to displace a specific radiolabeled ligand from GPR18 is measured to calculate its binding affinity. Functional assays, such as measuring calcium mobilization or cAMP accumulation, are used to confirm GPR18 activation and determine EC50 values.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK293-GPR18 cells Tested Concentrations: 0.1 nM-100 µM Incubation Duration: 5 min Experimental Results: Drove MAPK activation. In vitro cell-based assays are conducted using cells expressing GPR18. The cells are treated with N-arachidonylglycine, and receptor activation is measured by assessing downstream signaling events such as calcium mobilization or inhibition of cAMP accumulation. The compound's anti-inflammatory effects are evaluated by measuring the production of pro-inflammatory cytokines. |
| Animal Protocol |
Animal/Disease Models: Rats[3]
Doses: 10 mg/kg Route of Administration: Oral Experimental Results: Inhibition of FAAH, causing a reduction in the hydrolytic cleavage of anandamid. Animal/Disease Models: Mouse (peritonitis model)[3] Doses: 1.2 mg/kg Route of Administration: Oral; once Experimental Results: Resulted in a significant 70% reduction of peritoneal cells. In vivo animal studies with N-arachidonylglycine are conducted in models of inflammation and pain to evaluate its therapeutic potential. The compound is typically administered via intraperitoneal or intravenous injection. Its effects on inflammatory markers, pain responses, and immune cell function are assessed. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for N-arachidonylglycine. As an endogenous lipid, its ADME properties would be characterized by rapid metabolism.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for N-arachidonylglycine. As an endogenous compound, it is generally well-tolerated at physiological concentrations.
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| References |
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| Additional Infomation |
N-Arachidonic acid glycine is a bioactive derivative of arachidonic acid ethanolamine (anandamide). It is an N-acylglycine and fatty amide. Its function is related to arachidonic acid. It is the conjugate acid of N-arachidonic acid glycine ester. There are reports and relevant data regarding the existence of N-arachidonic acid glycine in the human body.
N-Arachidonylglycine (NA-Gly) is an endogenous lipoamino acid and a full agonist at GPR18 with an EC50 of 44.5 nM. It is an anti-inflammatory compound that does not activate CB1 or CB2 receptors, making it a selective tool for studying GPR18 signaling. N-Arachidonylglycine is a valuable research tool for studying the endocannabinoid system, inflammation, and immune regulation. The compound is not a drug and is strictly for research purposes. |
| Molecular Formula |
C22H35NO3
|
|---|---|
| Molecular Weight |
361.52
|
| Exact Mass |
361.261
|
| CAS # |
179113-91-8
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| PubChem CID |
5283389
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| Appearance |
White to yellow solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
560.9±50.0 °C at 760 mmHg
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| Flash Point |
293.0±30.1 °C
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| Vapour Pressure |
0.0±3.3 mmHg at 25°C
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| Index of Refraction |
1.508
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| LogP |
5.88
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
26
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| Complexity |
476
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)NCC(=O)O
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| InChi Key |
YLEARPUNMCCKMP-DOFZRALJSA-N
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| InChi Code |
InChI=1S/C22H35NO3/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-21(24)23-20-22(25)26/h6-7,9-10,12-13,15-16H,2-5,8,11,14,17-20H2,1H3,(H,23,24)(H,25,26)/b7-6-,10-9-,13-12-,16-15-
|
| Chemical Name |
2-[[(5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoyl]amino]acetic acid
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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: 100 mg/mL (276.61 mM)
Ethanol: 50 mg/mL (138.30 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.92 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7661 mL | 13.8305 mL | 27.6610 mL | |
| 5 mM | 0.5532 mL | 2.7661 mL | 5.5322 mL | |
| 10 mM | 0.2766 mL | 1.3830 mL | 2.7661 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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