Molecular structure of GW 842166X, CAS Number: 666260-75-9
GW 842166X (CAS 666260-75-9)
Alternate Names:
2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro-2H-pyran-4-yl)methyl]-4-(trifluoromethyl)-5-pyrimidinecarboxamide
Application:
GW 842166X is an agonist of the CB2 receptor
CAS Number:
666260-75-9
Molecular Weight:
449.3
Molecular Formula:
C18H17Cl2F3N4O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
A CB2 receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively.2 When administered orally to rats in the Freund′s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.2
GW 842166X (CAS 666260-75-9) References
- Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain. | Giblin, GM., et al. 2007. J Med Chem. 50: 2597-600. PMID: 17477516
- In vitro and in vivo characterization of A-796260: a selective cannabinoid CB2 receptor agonist exhibiting analgesic activity in rodent pain models. | Yao, BB., et al. 2008. Br J Pharmacol. 153: 390-401. PMID: 17994110
- Characterization of a cannabinoid CB2 receptor-selective agonist, A-836339 [2,2,3,3-tetramethyl-cyclopropanecarboxylic acid [3-(2-methoxy-ethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene]-amide], using in vitro pharmacological assays, in vivo pain models, and pharmacological magnetic resonance imaging. | Yao, BB., et al. 2009. J Pharmacol Exp Ther. 328: 141-51. PMID: 18931146
- Latest advances in cannabinoid receptor agonists. | Thakur, GA., et al. 2009. Expert Opin Ther Pat. 19: 1647-73. PMID: 19939187
- Design and evaluation of a novel fluorescent CB2 ligand as probe for receptor visualization in immune cells. | Petrov, RR., et al. 2011. Bioorg Med Chem Lett. 21: 5859-62. PMID: 21855337
- Selective cannabinoid receptor 2 modulators: a patent review 2009--present. | Riether, D. 2012. Expert Opin Ther Pat. 22: 495-510. PMID: 22537079
- Recent advances in the development of selective CB(2) agonists as promising anti-inflammatory agents. | Leleu-Chavain, N., et al. 2012. Curr Med Chem. 19: 3457-74. PMID: 22709008
- The agonist binding mechanism of human CB2 receptor studied by molecular dynamics simulation, free energy calculation and 3D-QSAR studies. | Chen, JJ., et al. 2013. Yao Xue Xue Bao. 48: 1436-49. PMID: 24358778
- Ligand-based virtual screening identifies a family of selective cannabinoid receptor 2 agonists. | Gianella-Borradori, M., et al. 2015. Bioorg Med Chem. 23: 241-63. PMID: 25487422
- Design, syntheses, structure-activity relationships and docking studies of coumarin derivatives as novel selective ligands for the CB2 receptor. | Han, S., et al. 2015. Eur J Med Chem. 93: 16-32. PMID: 25644673
- The central cannabinoid receptor type-2 (CB2) and chronic pain. | Shang, Y. and Tang, Y. 2017. Int J Neurosci. 127: 812-823. PMID: 27842450
- Developing pyridazine-3-carboxamides to be CB2 agonists: The design, synthesis, structure-activity relationships and docking studies. | Qian, HY., et al. 2017. Eur J Med Chem. 137: 598-611. PMID: 28651225
- CB2 Agonist GW842166x Protected against 6-OHDA-Induced Anxiogenic- and Depressive-Related Behaviors in Mice. | Liu, X., et al. 2022. Biomedicines. 10: PMID: 35892676
- Recent Advances on Type-2 Cannabinoid (CB2) Receptor Agonists and their Therapeutic Potential. | Gasperi, V., et al. 2023. Curr Med Chem. 30: 1420-1457. PMID: 36028971
- GW842166X Alleviates Osteoarthritis by Repressing LPS-mediated Chondrocyte Catabolism in Mice. | Huang, WR., et al. 2022. Curr Med Sci. 42: 1046-1054. PMID: 36178576
Inhibitor of:
LOC645188.Activator of:
CB2.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GW 842166X, 1 mg | sc-205338 | 1 mg | $28.00 | |||
GW 842166X, 5 mg | sc-205338A | 5 mg | $124.00 |