Catalog No.: PC-47097Not For Human Use, Lab Use Only.
LY2828360 is a potent CB2 receptor agonist with similar affinity for human and rat CB2 receptors with Ki of 40.3 nM and 36.7 nM, respectively, shows EC50 of 20.1 nM in [35S]-GTPγS assays.
LY2828360 is a potent CB2 receptor agonist with similar affinity for human and rat CB2 receptors with Ki of 40.3 nM and 36.7 nM, respectively, shows EC50 of 20.1 nM in [35S]-GTPγS assays.
LY2828360 displays no agonist activity for CB1 receptor (EC50>10 uM).
LY2828360 is a slowly acting but efficacious G protein–biased CB2 agonist, inhibiting cAMP accumulation and activating extracellular signal-regulated kinase 1/2 signaling while failing to recruit arrestin, activate inositol phosphate signaling, or internalize CB2 receptors.
LY2828360 shows good CNS penetration and potent oral activity in a preclinical model of joint pain induced by intra-articular monoiodoacetic acid.
LY2828360 (0.3 mg/kg p.o.) produces a dose-related reversal of pain using incapacitance testing, demonstrating equivalent efficacy to the nonsteroidal anti-inflammatory drug diclofenac in the monoiodoacetic acid model.
