High affinity and selective CB2
inverse agonist (Ki
= 0.6 nM). Exhibits >700-fold selectivity for CB2
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.
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.
Rinaldi-Carmona et al.
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-trimeth
Kotsikorou et al.
Gi protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB2: implication for intracellular signalization cross-regulation.
Bouaboula et al.
The citations listed below are publications that use Tocris products. Selected citations for SR 144528 include:
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