Cat. No. 5039
Chemical Name: 5-(4-Chloro-3-methylphenyl)-1-[(4-m
Biological ActivityHigh affinity and selective CB2 inverse agonist (Ki = 0.6 nM). Exhibits >700-fold selectivity for CB2 over CB1 receptors. Blocks the effects of CP 55,940 (Cat. No. 0949) on forskolin-sensitive adenylyl cyclase activity and MAPK in CHO cells expressing CB2 receptors. Also blocks CP 55,940-induced B-cell activation. Orally bioavailable.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Kotsikorou et al (2013) The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide (SR144528). J.Med.Chem. 56 6593. PMID: 23855811.
Bouaboula et al (1999) Gi protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB2: implication for intracellular signalization cross-regulation. Mol.Pharmacol. 55 473. PMID: 10051530.
Rinaldi-Carmona et al (1998) SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J.Pharmacol.Exp.Ther. 284 644. PMID: 9454810.
If you know of a relevant reference for SR 144528 please let us know.
Citations are publications that use Tocris products. Selected citations for SR 144528 include:
Shang et al (2016) & #916; 9-Tetrahydrocannabinol Reverses TNFα-induced Increase in Airway Epithelial Cell Permeability through CB 2 Receptors Biochemical Pharmacology. PMID: 27641813.
Presley et al (2015) Preclinical evaluation of SMM-189, a cannabinoid receptor 2-specific inverse agonist. J Neurosci 3 e00159. PMID: 26196013.
Do you know of a great paper that uses SR 144528 from Tocris? If so please let us know.
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