SR 144528

Key Product Details

Product Description

SR 144528 is a high affinity and selective CB₂ inverse agonist (K_i = 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.

Product Specifications for SR 144528

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for SR 144528

The following data is based on the product molecular weight 476.05.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.10 mL	10.50 mL	21.01 mL
5 mM	0.42 mL	2.10 mL	4.20 mL
10 mM	0.21 mL	1.05 mL	2.10 mL
50 mM	0.04 mL	0.21 mL	0.42 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 9 publications citing the usage of this product.

• Kotsikorou 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 J.Med.Chem. 2013 PMID: 23855811
• Bouaboula G_i protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB₂: implication for intracellular signalization cross-regulation. Mol.Pharmacol. 1999 PMID: 10051530
• Rinaldi-Carmona SR 144528, the first potent and selective antagonist of the CB₂ cannabinoid receptor. J.Pharmacol.Exp.Ther. 1998 PMID: 9454810

Product Documents for SR 144528