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Chemical Structure : SR144528
CAS No.: 192703-06-3
Catalog No.: PC-60753Not For Human Use, Lab Use Only.
SR144528 is a highly potent, selective and orally active antagonist of CB2 receptor with Ki of 0.6 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $98 | In stock | |
| 10 mg | $148 | In stock | |
| 25 mg | $258 | In stock | |
| 50 mg | $398 | In stock | |
| 100 mg | Get quote |
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SR144528 is a highly potent, selective and orally active antagonist of CB2 receptor with Ki of 0.6 nM.
SR144528 displays 700-fold lower affinity (Ki= 400 nM) for CB1 receptors, and no affinity for any of the more than 70 receptors, ion channels or enzymes (IC50>10 uM).
SR144528 antagonizes the inhibitory effects of CP 55,940 on forskolin-stimulated adenylyl cyclase activity with EC50 of 10 nM in cell-based assays, selectively blocks the MAPK activity induced by CP 55,940 with IC50 of 39 nM.
SR144528 displaces the ex vivo [3H]-CP 55,940 binding to mouse spleen membranes (ED50=0.35 mg/kg) with a long duration of action.
| M.Wt | 476.05 | |
| Formula | C29H34ClN3O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
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 |
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1. Rinaldi-Carmona M, et al. J Pharmacol Exp Ther. 1998 Feb;284(2):644-50.
2. Portier M, et al. J Pharmacol Exp Ther. 1999 Feb;288(2):582-9.
3. Carayon P, et al. Blood. 1998 Nov 15;92(10):3605-15.
4. Griffin G, et al. Eur J Pharmacol. 1999 Jul 14;377(1):117-25.
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