EG01449 is a specific, small molecule neuropilin-1 (NRP1) antagonist, inhibits bt-VEGFA to NRP1 b1 domain with IC50 of 362 nM, and SPR KD of 0.6 uM for binding to NRP1 b1 domain.
EG01449 (30 uM) inhibits VEGFA-induced permeability and signaling in models-vascular endothelial cells of the ex vivo mouse retina and human brain endothelial cells.
EG01449 (30 uM) prevents VEGFA-induced p38 phosphorylation in human brain endothelial cell line hCMEC/D3.
EG01449 (30 uM) significantly reduced VEGFA-induced dye extravasation in mouse brain and retinae.
EG01449 (30 uM) prevented the VEGFA-mediated increase in total sodium currents in DRG neurons.
EG01449 reduces VEGFA induced pain-like phenotype in male and female rats, blocks VEGFA-induced increase in aversion to mechanical stimuli in rats.
EG01449 does not activate p38 mitogen-activated protein kinase and exhibited a purely inhibitory pharmacological profile.