Biological Activity
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.
Technical Data
| M. Wt | 447.36 |
| Formula | C23H24Cl2N2O3 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 180002-83-9 |
| PubChem ID | 9911463 |
| InChI Key | FSFZRNZSZYDVLI-UHFFFAOYSA-N |
| Smiles | COC1=CC=C2N(C(=O)C3=C(Cl)C(Cl)=CC=C3)C(C)=C(CCN3CCOCC3)C2=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 22.36 | 50 | |
| ethanol | 22.37 | 50 |
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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.24 mL | 11.18 mL | 22.35 mL |
| 5 mM | 0.45 mL | 2.24 mL | 4.47 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.24 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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References
References are publications that support the products' biological activity.
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
Keywords: GW 405833, supplier, Selective, high, affinity, CB2, receptor, partial, agonists, cannabinoids, Receptors, GW405833, L768242, cb2r, L-768,242, CB2, Receptors, Tocris Bioscience
