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EG00229 is a neuropilin 1 (NRP1) receptor antagonist that selectively inhibits the binding of VEGF-A to the NRP1 b1 domain with an IC50 value of 3 μM. It does not affect the binding of VEGF-A to other receptors, such as VEGFR-1 and VEGFR-2.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $45 | In Stock | |
2 mg | $64 | In Stock | |
5 mg | $101 | In Stock | |
10 mg | $159 | In Stock | |
25 mg | $265 | In Stock | |
50 mg | $392 | In Stock | |
100 mg | $583 | In Stock | |
1 mL x 10 mM (in DMSO) | $143 | In Stock |
Description | EG00229 is a neuropilin 1 (NRP1) receptor antagonist that selectively inhibits the binding of VEGF-A to the NRP1 b1 domain with an IC50 value of 3 μM. It does not affect the binding of VEGF-A to other receptors, such as VEGFR-1 and VEGFR-2. |
Targets&IC50 | Bt-VEGF-A binding to purified NRP1 b1 domain:3 μM , [125I]-VEGF-A binding to PAE/NRP1:8 μM |
In vitro | EG00229 selectively inhibits radiolabeled 125I-VEGF-A binding to porcine aortic endothelial (PAE)/NRP1, but not VEGFR2-expressing cells, with an IC50 of 8 μM. EG00229 also inhibits VEGF-A binding to lung carcinoma A549 and prostate carcinoma DU145 cells, which express NRP1, but not VEGFR1 and VEGFR2, with similar potency. Binding of VEGF-A to human umbilical vein endothelial cells (HUVECs), which express VEGFR2, VEGFR1, and NRP1, is also inhibited by EG00229 with an IC50 of 23 μM.EG00229 ( 0-100 μM; 48 hours; A549 cells) treatment causes a significant reduction in cell viability over a 48 hours incubation. EG00229 demonstrates inhibition of VEGF-A binding to NRP1 and attenuates VEGFR2 phosphorylation in endothelial cells. Inhibition of migration of endothelial cells is also observed in HUVECs. |
In vivo | EG00229 treatment substantially reduces tumor growth and visible vascularization. |
Molecular Weight | 611.6 |
Formula | C19H20F3N7O7S3 |
Cas No. | 1210945-69-9 |
Smiles | OC(=O)C(F)(F)F.NC(=N)NCCC[C@H](NC(=O)c1sccc1NS(=O)(=O)c1cccc2nsnc12)C(O)=O |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 41.4 mg/mL (67.69 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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