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Potent and selective CB2 receptor partial agonist (EC50 = 0.65 nM; maximum inhibition = 44.6%). Binds with high affinity to both human and rat CB2 receptors and displays ~ 1200-fold selectivity over CB1 (Ki values are 3.92 and 4772 nM for human recombinant CB2 and CB1 receptors respectively). Produces potent antihyperalgesic effects in several rodent models of pain.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 447.36. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.47 mL||22.35 mL||44.71 mL|
|2.5 mM||0.89 mL||4.47 mL||8.94 mL|
|5 mM||0.45 mL||2.24 mL||4.47 mL|
|25 mM||0.09 mL||0.45 mL||0.89 mL|
References are publications that support the biological activity of the product.
Clayton et al (2002) CB1 and CB2 cannabinoid receptors are implicated in inflammatory pain. Pain 96 253 PMID: 11972997
Valenzano et al (2005) Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy. Neuropharmacology 48 658 PMID: 15814101
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Keywords: GW 405833, GW 405833 supplier, Selective, high, affinity, CB2, receptor, partial, agonists, cannabinoids, Receptors, GW405833, L768242, cb2r, L-768,242, 2374, Tocris Bioscience
4 Citations for GW 405833
Citations are publications that use Tocris products. Selected citations for GW 405833 include:
Schuelert et al (2010) Paradoxical effects of the cannabinoid CB2 receptor agonist GW405833 on rat osteoarthritic knee joint pain. Osteoarthritis Cartilage 18 1536 PMID: 20863899
Marini et al (2013) Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors. Br J Pharmacol 169 887 PMID: 23711022
McGuinness et al (2009) Characterizing cannabinoid CB2 receptor ligands using DiscoveRx PathHunter β-arrestin assay. Cardiovasc Res 14 49 PMID: 19171920
Li et al (2017) Cannabinoid CB2 Agonist GW405833 Suppresses Inflammatory and Neuropathic Pain through a CB1 Mechanism that is Independent of CB2 Receptors in Mice. J Pharmacol Exp Ther 362 296 PMID: 28592614
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Literature in this Area
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Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.