PD176252 is also an agonist of N-Formyl peptide receptor1/2 (EC50s: 0.31 and 0.66 μM in HL-60 cells). PD176252 is an effective antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor (Kis: 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively).

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

Rat BB1 receptor:0.66 nM(ki), Human BB2 receptor:1 nM(ki), FPR1:（EC50）0.31 μM, Human BB1 receptor:（ki）0.17 nM, FPR2:0.66 μM, Rat BB2 receptor:16 nM

PD176252 inhibits little specific 125I-gastrin-releasing peptide binding to NCI-H345 cells at 1 nM and suppresses almost all specific bindings at 1000 nM (IC50: 30 nM). PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C at the human BB1 or BB2 receptors expressed in CHO cells, with the appKBs of 4.0 nM or 13 nM, and blocks bombesin-evoked increases in intracellular calcium levels in CHO cells stably expressing human BB1 or BB2 receptors, with appKBs of 2.3 nM and 36 nM, respectively. PD176252 activates Ca2+ mobilization in HL-60 cells transfected with human FPRs (EC50, 0.72 ± 0.21 μM). PD176252 (10, 30 μM) significantly inhibits the growth of NCI-H345 or H1299 cells (IC50s: 7 and 5 μM) [2][3].

In nude mice, PD176252 (1, 10 μg, p.o.) effectively suppresses the growth of the proliferation of NCI-H1299 xenografts [3].