| 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 |
Cannabinoid-2 (CB2) receptor. GW405833 hydrochloride is a potent and selective CB2 receptor agonist. The CB2 receptor is primarily expressed in immune cells and is involved in modulating pain and inflammation. By activating CB2 receptors, GW405833 inhibits forskolin-stimulated cyclic adenosine monophosphate (cAMP) formation, leading to the modulation of intracellular signaling pathways involved in pain perception and inflammatory responses. Its high selectivity for CB2 over CB1 minimizes psychoactive side effects.
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| ln Vitro |
In vitro, GW405833 hydrochloride has been characterized using radioligand binding and functional assays. It binds to the CB2 receptor with high affinity (Ki = 3.6 nM) and shows excellent selectivity over the CB1 receptor (1200-fold). In functional assays, it acts as a partial agonist, inhibiting forskolin-stimulated cAMP accumulation with an EC50 of 0.65 nM and a maximum inhibition of 44.6%. These properties make it a valuable tool for studying CB2 receptor function.
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| ln Vivo |
In vivo, GW405833 hydrochloride exhibits significant antihyperalgesic effects in various rodent pain models. It has been studied for its potential to modulate metabolic processes, reduce insulin sensitivity, and alter lipid metabolism. It is used in research to study conditions such as type 2 diabetes, obesity, and cardiovascular diseases, as well as to evaluate potential therapeutic applications. Its efficacy in pain models confirms its in vivo activity as a CB2 agonist.
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| Enzyme Assay |
In vitro receptor binding assays for GW405833 hydrochloride involve radioligand binding to membrane preparations from cells expressing recombinant CB2 or CB1 receptors. The compound is incubated with a radiolabeled CB2 ligand (e.g., [3H]CP-55,940) and membrane preparations. Non-specific binding is determined in the presence of excess unlabeled ligand. The IC50 or Ki for displacement is calculated. Selectivity is confirmed by testing against CB1 receptors.
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| Cell Assay |
In vitro cell-based assays for GW405833 hydrochloride are performed in cells expressing recombinant CB2 receptors. cAMP accumulation assays are commonly used, where cells are treated with forskolin to stimulate cAMP production, and the inhibition of this production by GW405833 is measured. The EC50 and maximum inhibition are determined. Calcium mobilization assays can also be used. These assays confirm the functional agonism of the compound at the CB2 receptor.
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| Animal Protocol |
In vivo animal experiments with GW405833 hydrochloride have been conducted in various rodent pain models. Typically, rodents are administered the compound via oral or intraperitoneal injection, and pain responses are measured using models such as the formalin test, CFA-induced hyperalgesia, or neuropathic pain models. The compound's antihyperalgesic effects are compared to vehicle or standard treatments. These experiments demonstrate its in vivo efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GW405833 hydrochloride have been studied. As a small molecule with a hydrochloride salt form, it has enhanced solubility and stability. It is typically administered orally or intraperitoneally in animal studies. Its half-life, bioavailability, and metabolism are not detailed in the available literature. Its ability to cross the blood-brain barrier is likely limited due to its CB2 selectivity, as CB2 is primarily peripheral. Standard PK studies would be required for full characterization.
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| Toxicity/Toxicokinetics |
Toxicological data for GW405833 hydrochloride are not detailed in the available literature. It is a research compound not intended for human use. No LD50 values or repeated-dose toxicity studies have been reported. Standard safety pharmacology studies have not been performed. As with all research chemicals, appropriate safety precautions should be taken when handling. Its specific toxicity profile has not been established.
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| References |
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| Additional Infomation |
GW405833 hydrochloride is a potent and selective CB2 receptor agonist. It has an EC50 of 0.65 nM and a maximum inhibition of 44.6%. It exhibits significant antihyperalgesic effects in rodent pain models. It binds to CB2 with a Ki of 3.6 nM and shows 1200-fold selectivity over CB1. It is also known as L768242 hydrochloride. It is used in research for pain, inflammation, and metabolic disorders. It is available for research use only.
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| Molecular Formula |
C23H25CL3N2O3
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| Molecular Weight |
483.82
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| Exact Mass |
482.093
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| CAS # |
1202865-22-2
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| PubChem CID |
24849093
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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 |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
589
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C2=C(N1C(=O)C3=C(C(=CC=C3)Cl)Cl)C=CC(=C2)OC)CCN4CCOCC4.Cl
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| InChi Key |
JIQYDHDVNNFPMU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24Cl2N2O3.ClH/c1-15-17(8-9-26-10-12-30-13-11-26)19-14-16(29-2)6-7-21(19)27(15)23(28)18-4-3-5-20(24)22(18)25;/h3-7,14H,8-13H2,1-2H3;1H
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| Chemical Name |
(2,3-dichlorophenyl)-[5-methoxy-2-methyl-3-(2-morpholin-4-ylethyl)indol-1-yl]methanone;hydrochloride
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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, avoid exposure to moisture. |
| 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 :~125 mg/mL (~258.36 mM; with sonication (<60°C))
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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 | 2.0669 mL | 10.3344 mL | 20.6688 mL | |
| 5 mM | 0.4134 mL | 2.0669 mL | 4.1338 mL | |
| 10 mM | 0.2067 mL | 1.0334 mL | 2.0669 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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