| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
Neuropilin-1 (NRP-1) receptor. EG00229 TFA is a selective inhibitor that binds to the b1 domain of NRP-1. By blocking the interaction of NRP-1 with its ligands, such as VEGF-A and semaphorin 3A, it inhibits downstream signaling pathways involved in angiogenesis, cell migration, and tumor progression.
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| ln Vitro |
After 48 hours of incubation, treatment with EG00229 (Compound 2; 0-100 μM; 48 hours; A549 cells) significantly reduced the viability of the cells [1]. Compound 2 (EG00229) reduces endothelial cell VEGFR2 phosphorylation and prevents VEGF-A from attaching to NRP1. HUVEC have also shown evidence of inhibition of endothelial cell migration [1]. At an IC50 of 8 μM, EG00229 (compound 2) specifically prevents radiolabeled 125I-VEGF-A from binding to porcine aortic endothelium (PAE)/NRP1, but not to VEGFR2-expressing cells. EG00229 similarly decreased VEGF-A binding to prostate cancer DU145 and lung cancer A549 cells, which express NRP1 but not VEGFR1 or VEGFR2. EG00229, with an IC50 of 23 μM, also inhibits the binding of VEGF-A to human umbilical vein endothelial cells (HUVEC) expressing VEGFR2, VEGFR1, and NRP1 [1].
EG00229 TFA is a selective inhibitor of the NRP-1 receptor. It binds to the b1 domain of NRP-1 and inhibits the binding of VEGF-A to NRP-1. In vitro, it has been shown to inhibit VEGF-A-induced migration and tube formation in endothelial cells. It also inhibits the migration of cancer cells. |
| ln Vivo |
For four weeks, NSG mice treated with EG00229 (0–10 mg/kg; i.p.; three times per week) showed a significant decrease in tumor growth and evident vascularization [2].
In vivo, EG00229 TFA has been investigated for its anti-angiogenic and anti-tumor activity. It has been shown to inhibit tumor growth in xenograft models. Its effects are mediated through the inhibition of NRP-1 signaling, which reduces angiogenesis and tumor cell migration. |
| Enzyme Assay |
In vitro assays for EG00229 TFA involve measuring its binding to NRP-1. Surface plasmon resonance (SPR) or ELISA-based binding assays can be used to determine its affinity for the NRP-1 b1 domain. Its ability to inhibit the interaction between NRP-1 and its ligands, such as VEGF-A, can be assessed in competition assays.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: A549 Cell Tested Concentrations: 0 µM, 10 µM, 30 µM, 100 µM Incubation Duration: 48 hrs (hours) Experimental Results: Caused significant reduction in cell viability. In vitro cell-based assays for EG00229 TFA are performed to study its effects on angiogenesis and cell migration. Endothelial cells are treated with the compound, and their ability to form tubes in a Matrigel assay is assessed. Cell migration is measured using wound healing or Boyden chamber assays. The compound's effects on VEGF-induced signaling can also be measured. |
| Animal Protocol |
Animal/Disease Models: 6weeks old female NOD scid IL2 receptor gamma chain knockout mice (NSG mice) with ECS cells [2]
Doses: 0 mg/kg, 10 mg/kg Route of Administration: intraperitoneal (ip) injection; every Wednesday times; lasts 4 weeks Experimental Results: diminished tumor growth and visible blood vessel formation. In vivo animal studies for EG00229 TFA are conducted in xenograft models of cancer. Tumor-bearing mice are treated with the compound, and tumor growth is measured. The compound's effects on angiogenesis can be assessed by measuring tumor vascular density. Its pharmacokinetics and tolerability are also evaluated. |
| ADME/Pharmacokinetics |
EG00229 TFA has a molecular weight of 543.56 and a molecular formula of C24H28F3N3O6S. The TFA salt form is used to improve the compound's solubility and stability. It should be stored as powder at -20°C. For in vivo administration, it can be formulated in a suitable vehicle.
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| Toxicity/Toxicokinetics |
No specific toxicity data are documented for EG00229 TFA in the provided sources. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound.
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| References |
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| Additional Infomation |
EG00229 TFA is a selective inhibitor of the neuropilin-1 (NRP-1) receptor. It binds to the b1 domain of NRP-1 and blocks its interaction with VEGF and semaphorins. It has been investigated for its anti-angiogenic and anti-tumor activity. It is for research use only.
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| Molecular Formula |
C₁₉H₂₀F₃N₇O₇S₃
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|---|---|
| Molecular Weight |
611.595
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| Exact Mass |
611.054
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| CAS # |
1210945-69-9
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| Related CAS # |
1018927-63-3;1210945-69-9 (TFA);
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| PubChem CID |
45142253
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.368
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
39
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| Complexity |
901
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC2=NSN=C2C(=C1)S(=O)(=O)NC3=C(SC=C3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O.C(=O)(C(F)(F)F)O
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| InChi Key |
ZYQBITUOSRZDTG-MERQFXBCSA-N
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| InChi Code |
InChI=1S/C17H19N7O5S3.C2HF3O2/c18-17(19)20-7-2-4-11(16(26)27)21-15(25)14-10(6-8-30-14)24-32(28,29)12-5-1-3-9-13(12)23-31-22-93-2(4,5)1(6)7/h1,3,5-6,8,11,24H,2,4,7H2,(H,21,25)(H,26,27)(H4,18,19,20)(H,6,7)/t11-/m0./s1
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| Chemical Name |
N2-[[3-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-2-thienyl]carbonyl]-L-arginine trifluoroacetate
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| Synonyms |
EG 00229 trifluoroacetate, EG-00229 TFA, EG-00229 trifluoroacetate, EG00229 TFA,
EG00229 trifluoroacetate, EG 00229 TFA
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 41.4 mg/mL (~67.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6351 mL | 8.1753 mL | 16.3506 mL | |
| 5 mM | 0.3270 mL | 1.6351 mL | 3.2701 mL | |
| 10 mM | 0.1635 mL | 0.8175 mL | 1.6351 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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