PD176252 NLT 98%

PD176252 is a potent antagonist of neuromedin-B preferring (BB₁) and gastrin-releasing peptide-preferring (BB₂) receptor with K_is of 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; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC₅₀s of 0.31 and 0.66 μM in HL-60 cells. IC50 & Target: Ki: 0.17 nM (Human BB₁ receptor), 0.66 nM (Rat BB₁ receptor), 1 nM (Human BB₂ receptor), 16 nM (Rat BB₂ receptor)^[1]
EC50: 0.31 μM (FPR1), 0.66 μM (FPR2)^[2] In Vitro: PD176252 is a potent antagonist of neuromedin-B preferring (BB₁) and gastrin-releasing peptide-preferring (BB₂) receptor with K_is of 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. PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C at the human BB₁ or BB₂ receptors expressed in CHO cells, with the appK_Bs 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 appK_Bs of 2.3 nM and 36 nM, respectively. PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC₅₀s of 0.31 and 0.66 μM in HL-60 cells. PD176252 activates Ca²⁺ mobilization in HL-60 cells transfected with human FPRs (EC₅₀, 0.72 ± 0.21 μM)^[2]. 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, with an IC₅₀ of 30 nM. PD176252 (10, 30 μM) significantly inhibits the growth of NCI-H345 or H1299 cells, with IC₅₀s of 7 and 5 μM^[3]. In Vivo: PD176252 (1, 10 μg, p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice^[3].