| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
CB-25 binds with high affinity to both CB1 and CB2 cannabinoid receptors, with Ki values of 5.2 nM (CB1) and 13 nM (CB2). It acts as an inverse agonist at the CB1 receptor, as assessed in a cyclic AMP (cAMP) functional assay, meaning it reduces the constitutive activity of the receptor below its baseline level.
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|---|---|
| ln Vitro |
In vitro, CB-25 binds to both CB1 (Ki=5.2 nM) and CB2 (Ki=13 nM) receptors, demonstrating high affinity. It behaves as an inverse agonist for the CB1 receptor, reducing cAMP accumulation below baseline levels. In cancer cells (but not in hCB1-CHO cells), CB-25 enhances forskolin-induced cAMP formation, indicating a cell-specific and context-dependent pharmacological profile.
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| ln Vivo |
In vivo activity data for CB-25 is not detailed in these references. As a stable, high-affinity inverse agonist, it is likely used to study the effects of suppressing constitutive CB1 receptor activity in animal models. Its in vivo effects may be distinct from neutral antagonists, potentially producing different physiological outcomes in models of pain, feeding, or mood disorders.
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| Enzyme Assay |
The binding affinity of CB-25 is determined via radioligand competition binding assays. For CB1, rat brain cortical membranes are incubated with [3H]CP-55,940 (a high-affinity CB1 agonist) and varying concentrations of CB-25. For CB2, membranes from CHO cells expressing human recombinant CB2 receptors are used with the same radioligand. Incubations are performed at 30degC for 60 min, and bound radioactivity is measured after filtration.
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| Cell Assay |
Functional activity is assessed by measuring its effect on forskolin-stimulated cAMP accumulation. CHO cells stably expressing human CB1 receptors are treated with forskolin to elevate cAMP levels, then incubated with varying concentrations of CB-25. CB1 inverse agonists like CB-25 reduce the constitutive inhibitory tone on adenylyl cyclase, leading to a further decrease in cAMP production. cAMP levels are quantified by HTRF or ELISA.
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| Animal Protocol |
No specific in vivo animal protocol for CB-25 is described in the provided references. A typical protocol for a CB1 inverse agonist would involve oral or intraperitoneal administration to mice followed by standard behavioral tests for cannabinoid activity, such as the tetrad assay (measuring locomotor activity, body temperature, tail-flick latency, and catalepsy).
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for CB-25 is not provided. As a stable analog of anandamide, it is designed to be resistant to enzymatic hydrolysis by FAAH, which should prolong its in vivo half-life compared to the parent endocannabinoid. Its high lipophilicity (LogP is likely high due to its long alkyl chain) suggests it would be well-absorbed but may require formulation in lipid-based vehicles.
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| Toxicity/Toxicokinetics |
No detailed toxicological data is available. As a potent cannabinoid receptor ligand, CB-25 would be expected to produce the classic pharmacological effects of cannabinoids at high doses, which could be considered toxic in a research context (e.g., severe hypothermia, catalepsy, respiratory depression). Its safety profile in standard toxicology assays is not reported.
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| References | |
| Additional Infomation |
CB-25 is an aromatic ether.
CB-25 is unique because it is one of the few synthetic cannabinoids that exhibits high affinity for both CB1 and CB2 receptors while acting as an inverse agonist, not a neutral antagonist or agonist. The distinction between an inverse agonist and a neutral antagonist is crucial for understanding constitutive receptor activity, and CB-25 provides a tool to investigate this aspect of CB1 receptor biology. |
| Molecular Formula |
C25H41NO3
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|---|---|
| Molecular Weight |
403.60
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| Exact Mass |
403.308
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| CAS # |
869376-63-6
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| PubChem CID |
11654304
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| Appearance |
White to off-white solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
594.7±30.0 °C at 760 mmHg
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| Flash Point |
313.5±24.6 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.527
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| LogP |
6.91
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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 |
17
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| Heavy Atom Count |
29
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| Complexity |
424
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCC1=CC(=CC(=C1)OCCCCCCCCCCC(=O)NC2CC2)O
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| InChi Key |
XFHZHCKWTBGPFD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H41NO3/c1-2-3-10-13-21-18-23(27)20-24(19-21)29-17-12-9-7-5-4-6-8-11-14-25(28)26-22-15-16-22/h18-20,22,27H,2-17H2,1H3,(H,26,28)
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| Chemical Name |
N-cyclopropyl-11-(3-hydroxy-5-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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (247.77 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 | 2.4777 mL | 12.3885 mL | 24.7770 mL | |
| 5 mM | 0.4955 mL | 2.4777 mL | 4.9554 mL | |
| 10 mM | 0.2478 mL | 1.2389 mL | 2.4777 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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