EG00229

EG00229 is a small-molecule neuropilin-1 (NRP1) receptor antagonist. It selectively inhibits the binding of vascular endothelial growth factor A (VEGF-A) to the b1 domain of NRP1 with an IC50 of approximately 3 μM, without affecting VEGF-A binding to VEGFR-1 or VEGFR-2. By blocking the VEGF-A/NRP1 interaction, EG00229 attenuates VEGFR2 phosphorylation, inhibits downstream signaling, and reduces endothelial cell migration. It has been shown to decrease carcinoma cell viability, sensitize tumor cells to cytotoxic chemotherapeutics (such as paclitaxel and 5-fluorouracil), and inhibit arterial calcification in vivo. Additionally, EG00229 blocks tuftsin-mediated activation of NRP1 and prevents nerve growth factor (NGF)-induced sensitization of TRPV1 in sensory neurons.

Other names

EG00229 trifluoroacetateEG-00229 trifluoroacetateEG 00229 trifluoroacetateL-Arginine, N-[[3-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-2-thienyl]carbonyl]-, 2,2,2-trifluoroacetate (1:1)N2-[[3-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-2-thienyl]carbonyl]-L-arginine trifluoroacetate