SR144528 is an effective and selective antagonist of the CB2 receptor (Ki: 0.6 nM).

SR144528 inhibits microsomal acyl-coenzymeA: cholesterol acyltransferase (ACAT) activity in a concentration-dependent manner (IC50: 3.6±1.1 μM). SR144528 (10 μM) inhibits ACAT activities ~68%. SR144528 alone is able to stimulate in a concentration-dependent manner (EC50=26±6 nM, two experiments) the forskolin-sensitive adenylyl cyclase activity in CHO-CB2 cells with a maximum effect at 1 μM (4-fold stimulation) whereas at this concentration it has no significant effect on CHO-CB1 cells (15% inhibition). Raw 264.7 macrophages supplemented with SR144528 display reduced caspase-3 activity [1][2].

SR144528 does not induce any significant effect on gastrointestinal (GI) motility when given alone. SR144528 does not block but enhances delayed gastric emptying. No effect on the binding of [3H]-CP 55,940 to its specific sites in the brain is observed after either oral (up to 10 mg/kg) or i.c.v. (10 μg/animal) administration of SR144528 in mice. The occupancy by SR144528 of the spleen cannabinoid receptor is time-dependent and significant for at least 18 hours after oral administration at 3 mg/kg [1][3].

192703-06-3

C29H34ClN3O

476.05

DMSO:50 mg/mL (105.03 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years