| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
CB1
2-Palmitoylglycerol targets the cannabinoid CB1 receptor as a moderate agonist. It does not bind directly to cannabinoid receptors with high affinity, but rather potentiates the activity of 2-AG and other endocannabinoids to bind to CB1 and CB2 and inhibit adenylyl cyclase. The compound modestly internalizes CB1 receptor on its own at concentrations as low as 300 nM. It may also be an endogenous ligand for GPR119, suggesting multiple potential targets. |
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| ln Vitro |
At doses as low as 300 nM, 2-palmitoylglycerol (2-PG) weakly internalizes CB1 receptor on its own. 2. In the context of depolarization-induced suppression of excitation (DSE), palmitoylglycerol exhibits very little antagonistic behavior[1].
In vitro, 2-Palmitoylglycerol does not bind directly to cannabinoid receptors nor inhibit adenylyl cyclase. Instead, it potentiates the apparent binding of 2-AG and increases its ability to inhibit adenylyl cyclase. The compound modestly internalizes CB1 receptor on its own at concentrations as low as 300 nM. It is used in research to study the modulation of endocannabinoid signaling and the entourage effect, where multiple lipid mediators work together to produce physiological effects. |
| ln Vivo |
In vivo, 2-Palmitoylglycerol enhances the cannabinoid effects of 2-AG following combined administration with 2-linoleoylglycerol. This enhancement suggests that 2-Palmitoylglycerol acts as a positive modulator of endocannabinoid signaling in vivo. The compound may potentiate the analgesic, anti-inflammatory, and other effects of 2-AG. However, comprehensive in vivo studies of 2-Palmitoylglycerol alone are limited. The compound is used in research to study the entourage effect in the endocannabinoid system.
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| Enzyme Assay |
For non-cell-based receptor binding assays, 2-Palmitoylglycerol can be evaluated using membrane preparations from cells expressing CB1 or CB2 receptors. Radioligand binding displacement experiments are performed using [3H]-CP55940 or [3H]-WIN55212-2 as the radiolabeled ligand. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at 30°C for 60 minutes. Bound radioligand is separated from free by filtration through GF/B filters. Nonspecific binding is determined in the presence of excess unlabeled ligand. The lack of direct binding displacement would confirm the compound's modulatory mechanism.
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| Cell Assay |
For in vitro cellular assays, cells expressing CB1 or CB2 receptors are cultured in appropriate media. For adenylyl cyclase activity assays, cells are treated with 2-AG in the presence or absence of 2-Palmitoylglycerol. cAMP levels are measured using ELISA or HTRF-based detection. The compound's ability to potentiate 2-AG-induced inhibition of adenylyl cyclase is assessed. For receptor internalization assays, cells expressing fluorescently tagged CB1 receptors are treated with the compound and receptor internalization is measured by microscopy or flow cytometry.
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| Animal Protocol |
For in vivo animal studies, 2-Palmitoylglycerol can be administered to rodents via intraperitoneal injection, often in combination with 2-AG or 2-linoleoylglycerol. In cannabinoid effect models, parameters such as hypothermia, analgesia (hot plate or tail-flick tests), and catalepsy are measured following combined administration. The enhancement of 2-AG effects by 2-Palmitoylglycerol is assessed by comparing responses with and without the compound. Dosing regimens vary depending on the specific model and combination strategy.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of 2-Palmitoylglycerol have not been extensively characterized. As a fatty acid glycerol ester with a molecular weight of 330.51, it is expected to be highly lipophilic with good tissue penetration. The compound has a molecular formula of C19H38O4. Comprehensive ADME studies would be needed for full pharmacokinetic characterization. The compound is available for research use only.
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| Toxicity/Toxicokinetics |
The toxicity profile of 2-Palmitoylglycerol has not been extensively reported. As an endogenous fatty acid ester, it is expected to have a favorable safety profile at physiological concentrations. The compound is for research use only and not for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies.
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| References | |
| Additional Infomation |
2-Palmitoylglycerol is a 2-monoglyceride with a hexadecanoyl (palmitoyl) acyl group. It is an algal metabolite functionally related to hexadecanoic acid. 2-Monopalmitoylglycerol is found in or produced by Escherichia coli (strains K12 and MG1655). 2-Palmitoylglycerol has also been reported in Pinus massoniana, Nelumbo nucifera, and other organisms with relevant data.
2-Palmitoylglycerol (2-Palm-Gl) is a fatty acid glycerol ester and a congener of 2-arachidonoylglycerol (2-AG). It is a moderate CB1 agonist that does not bind directly to cannabinoid receptors but potentiates the activity of 2-AG. It enhances the in vivo cannabinoid effects of 2-AG and may be an endogenous ligand for GPR119. The compound is used in research to study the entourage effect in the endocannabinoid system. It is available for research purposes only. |
| Molecular Formula |
C19H38O4
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|---|---|
| Molecular Weight |
330.50
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| Exact Mass |
330.277
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| CAS # |
23470-00-0
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| PubChem CID |
123409
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| Appearance |
White to off-white solid powder
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| Density |
0.969g/cm3
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| Boiling Point |
460.6ºC at 760mmHg
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| Melting Point |
68-70°C
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| Flash Point |
150.8ºC
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| Index of Refraction |
1.4434 (estimate)
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| LogP |
4.364
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
23
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| Complexity |
252
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCCCCCCCCCC(=O)OC(CO)CO
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| InChi Key |
BBNYCLAREVXOSG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H38O4/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-19(22)23-18(16-20)17-21/h18,20-21H,2-17H2,1H3
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| Chemical Name |
1,3-dihydroxypropan-2-yl hexadecanoate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.0257 mL | 15.1286 mL | 30.2572 mL | |
| 5 mM | 0.6051 mL | 3.0257 mL | 6.0514 mL | |
| 10 mM | 0.3026 mL | 1.5129 mL | 3.0257 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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