| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Cannabinoid receptor 2 (CB2) as agonist; also acts as noncompetitive CB1 antagonist and lysosomal TRPML1 inhibitor.
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| ln Vitro |
GW405833 is a potent CB2 receptor agonist with an EC50 of 50.7 nM. It behaves as a noncompetitive CB1 antagonist. The compound partially reverses inflammation and hyperalgesia in animal models. It inhibits NLRP3 inflammasome activation and serves as a lysosomal TRPML1 specific inhibitor to validate TRPML1-mediated tau release in neurons.
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| ln Vivo |
In vivo, GW405833 inhibits inflammatory and neuropathic pain in animal models. It has been reported to partially reverse inflammation and hyperalgesia in models of acute inflammation. The compound also inhibits NLRP3 inflammasome activation in vivo. Specific dosing regimens and detailed efficacy data are available in preclinical literature.
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| Enzyme Assay |
CB2 receptor binding affinity is assessed using in vitro radioligand binding assays with membrane preparations from cells expressing recombinant CB2 receptors. Agonist activity is evaluated using cAMP inhibition assays or β-arrestin recruitment assays. Selectivity over CB1 is confirmed by parallel testing. TRPML1 inhibition is assessed using lysosomal calcium release assays.
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| Cell Assay |
Cellular activity is evaluated in immune cells such as macrophages or microglia for NLRP3 inflammasome inhibition. Neuronal cells are used for TRPML1-mediated tau release studies. Cells are treated with GW405833 at various concentrations and inflammatory cytokine release (IL-1β, IL-18), caspase-1 activation, or tau release is measured by ELISA or Western blot.
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| Animal Protocol |
In vivo efficacy is studied in rodent models of acute inflammation and neuropathic pain. GW405833 is administered via intraperitoneal or oral routes. Inflammatory hyperalgesia is assessed using paw withdrawal latency or von Frey filaments. NLRP3 inflammasome activation is evaluated by measuring IL-1β levels in serum or tissue. Dosing typically ranges from 1-30 mg/kg.
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| ADME/Pharmacokinetics |
GW405833 has a molecular formula of C23H24Cl2N2O3 and molecular weight of 447.36. Purity is typically ≥98% by HPLC. The compound is soluble in DMSO. Detailed pharmacokinetic parameters including half-life, oral bioavailability, and metabolic pathways are not extensively detailed in public search results.
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| Toxicity/Toxicokinetics |
Safety data indicate GW405833 is a research compound for laboratory use only. Specific toxicological profiles including acute toxicity, organ toxicity, and genotoxicity are not extensively published. As a CB2 agonist, it may have immune-modulating effects. Standard laboratory safety practices should be followed during handling.
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| References |
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| Additional Infomation |
(2,3-Dichlorophenyl)-[5-methoxy-2-methyl-3-[2-(4-morpholinyl)ethyl]-1-indolyl] methyl ketone is an N-acylindole.
GW405833 is a research tool compound for studying CB2 receptor biology, NLRP3 inflammasome, and TRPML1 function. It is not approved for clinical use. The compound has been investigated for pain, inflammation, and neurodegenerative disease research. Its dual activity as CB2 agonist and TRPML1 inhibitor makes it a valuable pharmacological probe. |
| Molecular Formula |
C23H24CL2N2O3
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|---|---|
| Molecular Weight |
447.35
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| Exact Mass |
446.116
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| CAS # |
180002-83-9
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| PubChem CID |
9911463
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| Appearance |
Light yellow to yellow solid powder
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| Melting Point |
47-49°C(lit.)
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| LogP |
4.766
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
589
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FSFZRNZSZYDVLI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24Cl2N2O3/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
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| Chemical Name |
(2,3-dichlorophenyl)-[5-methoxy-2-methyl-3-(2-morpholin-4-ylethyl)indol-1-yl]methanone
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| Synonyms |
L 768242; L768242; L-768242
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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 : ~125 mg/mL (~279.42 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 | 2.2354 mL | 11.1769 mL | 22.3539 mL | |
| 5 mM | 0.4471 mL | 2.2354 mL | 4.4708 mL | |
| 10 mM | 0.2235 mL | 1.1177 mL | 2.2354 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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