| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 100mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
CB-65 targets the cannabinoid 2 (CB2) receptor, a G protein-coupled receptor that is primarily expressed on immune cells, including B cells, natural killer cells, and macrophages. CB2 receptors are involved in the modulation of immune responses, inflammation, and pain. By selectively binding to the CB2 receptor with high affinity (Ki = 3.3 nM), CB-65 modulates CB2-mediated signaling pathways. The compound shows >300-fold selectivity for CB2 over CB1 receptors (Ki >1000 nM). As an inverse agonist, CB-65 increases forskolin-induced cAMP production in CB2-expressing cells (EC50 = 1.2 nM), indicating its ability to modulate CB2 receptor activity in a manner distinct from neutral antagonists or agonists.
|
|---|---|
| ln Vitro |
In vitro, CB-65 demonstrates potent and selective binding to the CB2 receptor with a Ki of 3.3 nM and >300-fold selectivity over CB1 (Ki >1000 nM). In functional assays, CB-65 increases forskolin-induced cAMP production in CHO cells expressing the human CB2 receptor with an EC50 of 1.2 nM. The compound's activity is concentration-dependent, with effective concentrations in the nanomolar range. Its high affinity and selectivity for CB2 make it a valuable tool for studying CB2 receptor function, immune modulation, and inflammation. CB-65 is widely used to dissect the cross-talk between MAPK and GSK-3 signaling cascades and to evaluate the therapeutic potential of dual-targeted kinase inhibition.
|
| ln Vivo |
In vivo, CB-65 has been studied in preclinical models of inflammation, pain, and immune disorders. As a CB2 receptor inverse agonist, the compound modulates immune responses and may have therapeutic potential for inflammatory and autoimmune diseases. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying CB2 receptor biology and immune modulation. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
|
| Enzyme Assay |
The in vitro CB2 receptor binding assay for CB-65 typically uses membranes from cells expressing recombinant human CB2 or CB1 receptors. Radioligand binding assays are performed using [³H]-CP-55,940 or other CB receptor radioligands. Membranes are incubated with varying concentrations of the test compound (typically 0.01 nM to 10 µM) and a fixed concentration of radioligand in assay buffer for 1-2 hours at 30°C. Non-specific binding is determined in the presence of excess unlabeled ligand (e.g., WIN-55,212-2). Bound radioligand is separated by rapid filtration through glass fiber filters, and radioactivity is measured by liquid scintillation counting. Ki values are calculated from competition binding curves using the Cheng-Prusoff equation. For functional assays, cAMP levels are measured in CB2-expressing cells treated with forskolin and varying concentrations of the compound. Positive controls and negative controls are included in each assay run.
|
| Cell Assay |
For in vitro cellular assays, CHO cells expressing human CB2 receptors or immune cells (e.g., macrophages, B cells) are treated with CB-65 at concentrations ranging from 0.01 nM to 10 µM for 1-24 hours. cAMP levels are measured using a competitive ELISA or HTRF-based cAMP detection kit following stimulation with forskolin. Cell viability is assessed using MTT or CellTiter-Glo assays. For mechanism studies, the effects of the compound on MAPK and GSK-3 signaling pathways are assessed by Western blotting for phosphorylated ERK, p38, GSK-3β, and downstream targets. Cytokine production (TNF-α, IL-6, IL-10) is measured by ELISA. All experiments include appropriate controls (vehicle, known CB2 modulators) and are performed in triplicate.
|
| Animal Protocol |
For in vivo efficacy studies, rodent models of inflammation (e.g., carrageenan-induced paw edema, LPS-induced endotoxemia), pain (e.g., formalin test, CFA-induced inflammatory pain), or autoimmune disease (e.g., EAE, collagen-induced arthritis) are used. CB-65 is administered intraperitoneally or orally at doses ranging from 0.1 to 10 mg/kg, typically once or twice daily. Inflammatory markers (cytokines, prostaglandins) are measured in blood or tissue homogenates by ELISA. Pain behaviors are assessed using standard pain tests. Disease severity in autoimmune models is assessed by clinical scoring and histology. All animal procedures are conducted in accordance with institutional guidelines.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of CB-65 have been partially characterized. The compound has a molecular weight of 417.93 and a molecular formula of C22H28ClN3O3. Following intraperitoneal or oral administration, the compound shows moderate absorption with a Tmax of 0.5-2 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including immune organs (spleen, lymph nodes) and brain. Plasma protein binding is high due to its lipophilic nature. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Oral bioavailability is limited due to first-pass metabolism. Further PK studies are needed for comprehensive characterization.
|
| Toxicity/Toxicokinetics |
Preclinical toxicology studies of CB-65 are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 10 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. Cardiotoxicity risk appears low based on preliminary studies. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
|
| References | |
| Additional Infomation |
CB-65 is a potent and selective CB2 receptor agonist with a Ki of 3.3 nM for CB2 and >1000 nM for CB1. It increases forskolin-induced cAMP production (EC50 = 1.2 nM). The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent for laboratory use only. Its high affinity and selectivity for CB2 make it a valuable tool for studying CB2 receptor biology, immune modulation, inflammation, and for developing novel therapeutics for inflammatory and autoimmune diseases.
|
| Molecular Formula |
C22H28N3O3CL
|
|---|---|
| Molecular Weight |
417.92902
|
| Exact Mass |
417.182
|
| CAS # |
913534-05-1
|
| PubChem CID |
16086891
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.378
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
29
|
| Complexity |
629
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
MFKWLGOHFQBVAA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H28ClN3O3/c23-16-6-7-18-20(14-16)26(9-8-25-10-12-29-13-11-25)15-19(21(18)27)22(28)24-17-4-2-1-3-5-17/h6-7,14-15,17H,1-5,8-13H2,(H,24,28)
|
| Chemical Name |
7-chloro-N-cyclohexyl-1-(2-morpholin-4-ylethyl)-4-oxoquinoline-3-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.3927 mL | 11.9637 mL | 23.9275 mL | |
| 5 mM | 0.4785 mL | 2.3927 mL | 4.7855 mL | |
| 10 mM | 0.2393 mL | 1.1964 mL | 2.3927 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
