| 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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| Other Sizes |
| Targets |
CB1 agonist 1 targets the cannabinoid receptor type 1 (CB1). The compound shows affinity for the CB1 receptor with a pIC50 value of 5.7. CB1 receptors are primarily located in the brain and central nervous system and are involved in the regulation of pain, inflammation, appetite, and mood. By activating CB1 receptors, the compound modulates neurotransmitter release and downstream signaling pathways. The compound is selective for CB1 over other receptor targets.
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| ln Vitro |
In vitro, CB1 agonist 1 demonstrates potent agonistic activity at the CB1 receptor with a pIC50 of 5.7. The compound activates CB1 receptor signaling pathways, leading to downstream effects on neurotransmitter release and neuronal excitability. Standard in vitro assays include receptor binding studies, [35S]GTPγS binding assays for G protein activation, and cAMP accumulation assays. The compound's potency at CB1 makes it a useful tool for studying CB1 receptor function in various cell-based systems.
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| ln Vivo |
In vivo, CB1 agonist 1 has been studied in animal models of brain disorders, pain, and inflammation. As a CB1 agonist, it may produce effects similar to those of endogenous cannabinoids, including analgesia, anti-inflammatory effects, and modulation of cognitive function. CB1 receptor activation in the brain can also produce psychoactive effects. The compound is used in preclinical research to explore therapeutic strategies for various conditions. However, comprehensive in vivo efficacy data from published literature are limited.
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| Enzyme Assay |
For non-cell-based receptor binding assays, CB1 agonist 1 can be evaluated using membrane preparations from cells expressing human 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 10 µM unlabeled CP55940. Ki or IC50 values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human CB1 receptors (e.g., CHO or HEK293 cells) are cultured in appropriate media. For G protein activation assays, [35S]GTPγS binding is measured. Membrane preparations are incubated with GDP, [35S]GTPγS, and various concentrations of CB1 agonist 1. The amount of bound [35S]GTPγS is measured by filtration. For cAMP accumulation assays, cells are pre-incubated with forskolin to stimulate cAMP production, then treated with various concentrations of the compound. cAMP levels are measured using ELISA or HTRF-based detection. For β-arrestin recruitment assays, BRET or enzyme complementation technology is used.
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| Animal Protocol |
For in vivo animal studies, CB1 agonist 1 is typically administered to rodents via intraperitoneal injection or oral gavage. In pain models (e.g., formalin test, hot plate test, or tail-flick test), nociceptive responses are measured following compound administration. In inflammation models (e.g., carrageenan-induced paw edema), inflammatory markers and paw swelling are assessed. In models of brain disorders (e.g., anxiety or depression models), behavioral tests are performed. Dosing regimens vary depending on the specific model.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of CB1 agonist 1 have not been extensively characterized. Based on its molecular weight of 452.52 and lipophilic structure, the compound is expected to have good oral absorption and blood-brain barrier penetration. The compound is available in DMSO solution for research use. It should be stored at -20°C for long-term stability. 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 CB1 agonist 1 has not been extensively reported. As a CB1 agonist, potential adverse effects may include those associated with cannabinoid receptor activation, such as sedation, hypothermia, cognitive impairment, and psychoactive effects. 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 cardiovascular function.
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| References | |
| Additional Infomation |
CB1 agonist 1 (compound 22) is a potent CB1 receptor agonist with a pIC50 of 5.7. The compound has a molecular weight of 452.52 and a molecular formula of C24H24N2O5S. Its chemical name is N-(4-methyl-3-(morpholinosulfonyl)phenyl)-2-phenoxybenzamide. CB1 agonist 1 is used in research to study brain disorders, pain, and inflammation. The compound is designed to selectively target CB1 receptors, which are primarily found in the brain and central nervous system. It is available for research purposes only and is not approved for clinical use.
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| Molecular Formula |
C24H24N2O5S
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| Molecular Weight |
452.52
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| Exact Mass |
452.141
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| CAS # |
851212-80-1
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| PubChem CID |
4880561
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| Appearance |
White to off-white solid powder
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| LogP |
5.463
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
712
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C=C(C=C1)NC(=O)C2=CC=CC=C2OC3=CC=CC=C3)S(=O)(=O)N4CCOCC4
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| InChi Key |
HASYDUIFQCRDMA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H24N2O5S/c1-18-11-12-19(17-23(18)32(28,29)26-13-15-30-16-14-26)25-24(27)21-9-5-6-10-22(21)31-20-7-3-2-4-8-20/h2-12,17H,13-16H2,1H3,(H,25,27)
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| Chemical Name |
N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-2-phenoxybenzamide
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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: 250 mg/mL (552.46 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 | 2.2098 mL | 11.0492 mL | 22.0985 mL | |
| 5 mM | 0.4420 mL | 2.2098 mL | 4.4197 mL | |
| 10 mM | 0.2210 mL | 1.1049 mL | 2.2098 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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