| 货号 | 5039/50 |
| 别名 | 5-(4-Chloro-3-methylphenyl)-1-[(4-m |
| 供应商 | Tocris |
| 生物活性 | High 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. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 476.05 |
| 分子式 | C29H34ClN3O |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
| 参考文献 | Kotsikorouet 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. Bouaboulaet 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-Carmonaet al (1998) SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J.Pharmacol.Exp.Ther. 284 644. PMID: 9454810. |