| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
CB1/2 agonist 3 targets the cannabinoid receptors CB1 and CB2, which are G protein-coupled receptors (GPCRs). CB1 receptors are predominantly expressed in the central nervous system, while CB2 receptors are mainly found on immune cells. As a competitive agonist, it binds to these receptors and activates them. This activation triggers downstream signaling pathways, including inhibition of adenylyl cyclase and modulation of ion channels, leading to various physiological effects.
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| ln Vitro |
CB1/2 agonist 3 (compound 52) has the ability to partially stimulate [35S]GTPγS binding to the hCB1-CHO cell membrane (EC50 value of 30.99 nM) and slightly decrease [35S]GTPγS binding to the hCB2-CHO cell membrane (EC50 value of 1.28 nM on average[1]. With a Kb value of 78.17 nM, CB1/2 agonist 3 (compound 52) exhibits antagonistic effects on the CB1/CB2 agonist CP-55940 (1 μM, 1 h)[1].
In vitro, CB1/2 agonist 3 is characterized by its binding affinity to human CB1 and CB2 receptors. It has Ki values of 5.9 nM for hCB1 and 3.5 nM for hCB2, indicating its high potency. These values are typically determined in radioligand binding assays. Functional assays, such as measuring inhibition of cAMP accumulation, confirm its agonist activity. |
| ln Vivo |
Specific in vivo activity data for CB1/2 agonist 3 are not provided in the available sources. As a potent cannabinoid receptor agonist, it would be expected to produce effects typical of cannabinoid receptor activation, such as analgesia, anti-inflammatory effects, and modulation of appetite. However, no specific studies are described.
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| Enzyme Assay |
A cell-free assay for CB1/2 agonist 3 would involve measuring its binding affinity to CB1 and CB2 receptors using radioligand binding assays. Membrane preparations containing the receptors are incubated with a radiolabeled antagonist and varying concentrations of the compound. The concentration required to displace 50% of the specific binding (IC50) is determined, and the Ki is calculated using the Cheng-Prusoff equation. For this compound, the Ki values are 5.9 nM (hCB1) and 3.5 nM (hCB2).
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| Cell Assay |
Cellular assays for CB1/2 agonist 3 typically involve measuring its ability to activate cannabinoid receptor signaling. Cells expressing CB1 or CB2 receptors are treated with the compound, and the inhibition of forskolin-stimulated cAMP accumulation is measured. The compound's potency (EC50) in this functional assay can be determined. These assays confirm its activity as an agonist.
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| Animal Protocol |
In vivo animal experiments for CB1/2 agonist 3 are not described in the available sources. As a research compound, it could be evaluated in animal models of pain, inflammation, or other conditions where cannabinoid receptors are involved. However, no specific protocols or data are provided.
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| ADME/Pharmacokinetics |
CB1/2 agonist 3 has a molecular formula and weight that are not specified in the sources. It is a small molecule. Specific pharmacokinetic parameters are not provided. As a research compound, it is intended for preclinical studies.
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| Toxicity/Toxicokinetics |
Toxicity data for CB1/2 agonist 3 are not provided in the available sources. As a research compound, it is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be observed.
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| References | |
| Additional Infomation |
CB1/2 agonist 3 (CAS: 2772655-86-2) is a potent non-selective cannabinoid receptor agonist. It is also known as Compound 52. The compound has high affinity for both CB1 and CB2 receptors with Ki values of 5.9 nM and 3.5 nM, respectively. It is a competitive agonist and is used in research to study the endocannabinoid system.
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| Exact Mass |
387.314
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| CAS # |
2772655-86-2
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| PubChem CID |
156020907
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| Appearance |
White to off-white solid powder
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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 |
17
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| Heavy Atom Count |
28
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| Complexity |
394
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCC1=CC(=CC=C1)OCCCCCCCCCCC(=O)NC2CC2
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| InChi Key |
ZWANZUMSTXYAJD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H41NO2/c1-2-3-10-14-22-15-13-16-24(21-22)28-20-12-9-7-5-4-6-8-11-17-25(27)26-23-18-19-23/h13,15-16,21,23H,2-12,14,17-20H2,1H3,(H,26,27)
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| Chemical Name |
N-cyclopropyl-11-(3-pentylphenoxy)undecanamide
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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 : ~10 mg/mL (~25.80 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1 mg/mL (2.58 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (2.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (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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