Agonist activity at C3a receptor in human MDM cells assessed as induction of intracellular calcium release measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
Antagonist activity at C5a receptor in human MDM cells assessed as inhibition of C5a-induced intracellular calcium release preincubated for 30 mins followed by C5a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
Stability of the compound in rat liver microsomes assessed as compound degradation at 1 uM preincubated for 5 mins followed by NADPH addition and measured after 1 hr by LC-MS/MS analysis
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
Potency index, ratio of SB290157 IC50 to test compound IC50 for antagonist activity at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release
Antiinflammatory activity in Wistar rat model of BR103-induced paw edema assessed as reduction in hind paw swelling at 10 mg/kg, po administered via gavage pretreated for 2 hrs followed by BR103 challenge and measured after 30 mins by digital caliper method relative to control