| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 50mg |
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| 100mg |
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| 500mg | |||
| Other Sizes |
| Targets |
CB2R 14.8 nM (Ki) CB2R 123.6 nM (EC50) CB1R 241.3 nM (Ki) CB1R 489 nM (EC50)
CB2R/FAAH modulator-1 targets the cannabinoid type 2 receptor (CB2R) as a full agonist and the fatty acid amide hydrolase (FAAH) as an inhibitor. It shows selectivity for CB2R (Ki = 14.8 nM) over CB1R (Ki = 241.3 nM). FAAH is the primary enzyme responsible for the degradation of endocannabinoids such as anandamide. By inhibiting FAAH, the compound increases endocannabinoid levels, while CB2R agonism directly activates CB2 receptor signaling. This dual mechanism may produce synergistic anti-inflammatory effects. |
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| ln Vitro |
In unstimulated monocytes and macrophages, CB2R/FAAH modulator-1 (Compound 13; 10 μM; 24 hours) decreases the production of pro-inflammatory cytokines TNFα, IFN-γ, IL-1β, and IL6 [1].
In vitro, CB2R/FAAH modulator-1 acts as a full agonist at CB2R and inhibits FAAH with an IC50 of 4 µM. At 10 µM for 24 hours, the compound decreases the production of pro-inflammatory cytokines TNFα, IFN-γ, IL-1β, and IL-6 in unstimulated monocytes and macrophages. The compound shows selectivity for CB2R over CB1R, with approximately 16-fold selectivity. Standard in vitro assays include receptor binding studies, FAAH enzyme activity assays, and measurement of cytokine production by ELISA or multiplex assays. |
| ln Vivo |
In vivo, CB2R/FAAH modulator-1 has been studied in inflammation models. The compound's dual mechanism (CB2R agonism + FAAH inhibition) is expected to produce synergistic anti-inflammatory effects. CB2R activation reduces inflammatory responses, while FAAH inhibition increases endocannabinoid levels, further modulating inflammation. However, comprehensive in vivo efficacy data from published literature are limited. The compound is used in preclinical research to study inflammatory diseases.
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| Enzyme Assay |
For non-cell-based receptor binding assays, CB2R/FAAH modulator-1 can be evaluated using membrane preparations from cells expressing human CB2 or CB1 receptors. Radioligand binding displacement experiments are performed using [3H]-CP55940 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. Ki values are calculated from displacement curves. For FAAH inhibition, enzyme activity assays are performed.
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| Cell Assay |
For in vitro cellular assays, monocytes or macrophages are cultured in appropriate media. Cells are treated with CB2R/FAAH modulator-1 at 10 µM for 24 hours. Cytokine production (TNFα, IFN-γ, IL-1β, IL-6) is measured in cell culture supernatants using ELISA or multiplex bead-based assays. For CB2R functional assays, cells expressing CB2 receptors are treated with the compound and [35S]GTPγS binding or cAMP accumulation is measured to confirm agonist activity. For FAAH inhibition assays, recombinant FAAH enzyme is incubated with the compound and a fluorogenic substrate, and enzyme activity is measured.
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| Animal Protocol |
For in vivo animal studies, CB2R/FAAH modulator-1 can be administered to rodents via intraperitoneal or oral administration. In inflammation models (e.g., carrageenan-induced paw edema, complete Freund's adjuvant-induced arthritis, or LPS-induced systemic inflammation), inflammatory markers, paw swelling, and cytokine levels are assessed. In pain models, nociceptive responses are measured. Dosing regimens vary depending on the specific model. Blood and tissue samples may be collected for pharmacokinetic and pharmacodynamic analysis.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of CB2R/FAAH modulator-1 have not been extensively characterized. Based on its molecular properties, the compound is expected to have moderate lipophilicity and good oral bioavailability. The compound is available in DMSO solution for research use. Comprehensive ADME studies would be needed for full pharmacokinetic characterization, including assessment of oral bioavailability, half-life, protein binding, and tissue distribution.
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| Toxicity/Toxicokinetics |
The toxicity profile of CB2R/FAAH modulator-1 has not been extensively reported. As a CB2R agonist and FAAH inhibitor, potential adverse effects may include those associated with cannabinoid receptor activation and elevated endocannabinoid levels. The compound is for research use only and not for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of effects on the central nervous system and immune function.
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| References | |
| Additional Infomation |
CB2R/FAAH modulator-1 (compound 13) is a dual-targeting compound that acts as a CB2R full agonist (Ki = 14.8 nM) and a FAAH inhibitor (IC50 = 4 µM). It shows approximately 16-fold selectivity for CB2R over CB1R. The compound reduces pro-inflammatory and increases anti-inflammatory cytokine production in monocytes and macrophages. It is used in inflammation research and is available for research purposes only.
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| Molecular Formula |
C24H27NO2
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|---|---|
| Exact Mass |
361.204
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| CAS # |
928892-60-8
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| PubChem CID |
17649671
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
5.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
497
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C2CC3CC1CC(C2)(C3)NC(=O)C4=CC=CC=C4OCC5=CC=CC=C5
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| InChi Key |
PXQAGCHSGRCYSI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H27NO2/c26-23(25-24-13-18-10-19(14-24)12-20(11-18)15-24)21-8-4-5-9-22(21)27-16-17-6-2-1-3-7-17/h1-9,18-20H,10-16H2,(H,25,26)
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| Chemical Name |
N-(1-adamantyl)-2-phenylmethoxybenzamide
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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.) |
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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