| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 609 nM (NRP1-a1 and NRP1-b)[1]
Neuropilin-1 (NRP1). EG01377 dihydrochloride is a potent, bioavailable, and selective inhibitor of NRP1. It binds to NRP1 with a Kd of 1.32 μM and inhibits NRP1-a1 and NRP1-b1 with IC50 values of 609 nM. NRP1 is a receptor for class 3 semaphorins and vascular endothelial growth factor (VEGF) and plays a critical role in angiogenesis and tumor progression. |
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| ln Vitro |
Vascular endothelial growth factor A (VEGF-A) induced tyrosine phosphorylation of VEGF-R2/KDR is inhibited by EG01377 (3-30 μM; 30 minutes)[1]. VEGFA can considerably lessen HUVEC cell migration when EG01377 (30 μM) is applied[1]. EG01377 (30 μM; 5 days) can postpone the closure of wounds caused by VEGF[1]. The network area, length, and branching points are all decreased by EG01377 (30 μM)[1]. EG01377 (30 μM; 7 days) inhibits angiogenesis produced by VEGF [1]. When combined with VEGFA, EG01377 (30 μM; 7 days) decreases the growth of A375P (malignant melanoma) spheroid outgrowth[1]. When tumor cell-derived factors are present, EG01377 (500 nM; 2 hours) prevents Nrp1+ regulatory T-cell SMAD3/AKT (Tregs) from producing transforming growth factor beta (TGFβ)[1].
EG01377 dihydrochloride is a potent NRP1 inhibitor with a Kd of 1.32 μM and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. By blocking NRP1, it inhibits VEGF-mediated angiogenesis and other NRP1-dependent signaling pathways. This makes it a valuable tool for studying the role of NRP1 in cancer, cardiovascular disease, and other disorders. |
| ln Vivo |
EG01377 (2 mg/kg; iv) has a promising half-life of 4.29 h, long enough to support treatment once daily in mice[1].
In vivo, EG01377 dihydrochloride is used to study the role of NRP1 in various diseases. By inhibiting NRP1, it can block angiogenesis and tumor growth. Its anti-angiogenic activity makes it a promising compound for cancer research. It is also used to study the role of RAGE in metabolic disorders and neurodegeneration. |
| Enzyme Assay |
The in vitro activity of EG01377 dihydrochloride against NRP1 is typically assessed using binding assays, such as surface plasmon resonance, to determine its affinity (Kd). Functional assays, such as VEGF-induced endothelial cell migration or tube formation assays, are used to confirm its inhibitory activity. The IC50 values are determined from these functional assays.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Human umbilical vein endothelial cells (HUVECs) Tested Concentrations: 3, 10 , 30 μM Incubation Duration: 30 minutes Experimental Results: Inhibited VEGF-A stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC50 of 30 μM. Cellular assays for EG01377 dihydrochloride involve treating cells that express NRP1, such as endothelial cells or cancer cells, with the compound. The inhibition of NRP1-mediated signaling, such as VEGF-induced cell migration or proliferation, is measured. This confirms that the compound can effectively inhibit NRP1 function in a cellular context. |
| Animal Protocol |
Animal/Disease Models: 6-8 week-old BABL/c female mice[1]
Doses: 2 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Iv administration Experimental Results: The half time (T1/2) of 4.29 h. In vivo efficacy of EG01377 dihydrochloride is evaluated in animal models of cancer, angiogenesis, or other NRP1-related diseases. The compound is administered, and its effects on tumor growth, vascularization, and disease progression are assessed. Its bioavailability makes it suitable for in vivo studies. |
| ADME/Pharmacokinetics |
EG01377 dihydrochloride is a small molecule with the molecular formula C26H32Cl2N6O6S2 and a molecular weight of 659.60. Its pharmacokinetic properties, such as oral bioavailability, make it a valuable tool for in vivo studies. It is a potent and selective NRP1 inhibitor.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for EG01377 dihydrochloride. As an inhibitor of NRP1, which is involved in angiogenesis and other critical processes, its toxicity profile would be an important consideration. Potential toxicities could be related to its anti-angiogenic effects. Standard preclinical safety studies would be required.
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| References | |
| Additional Infomation |
EG01377 dihydrochloride (CAS#: 2749438-61-5) is a potent, bioavailable, and selective inhibitor of neuropilin-1 (NRP1). It has a Kd of 1.32 μM and IC50s of 609 nM for NRP1-a1 and NRP1-b1. It is a research tool for studying NRP1 in angiogenesis, cancer, and other diseases. It is not approved for clinical use.
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| Molecular Formula |
C26H32CL2N6O6S2
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|---|---|
| Molecular Weight |
659.604881286621
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| Exact Mass |
658.12
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| CAS # |
2749438-61-5
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| Related CAS # |
EG01377;2227996-00-9
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| PubChem CID |
146681179
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
42
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| Complexity |
1010
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1COC2=C1C=C(C=C2S(=O)(=O)NC3=C(SC=C3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C4=CC=C(C=C4)CN.Cl.Cl
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| InChi Key |
ZYFLTIBQQSYBQT-FJSYBICCSA-N
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| InChi Code |
InChI=1S/C26H30N6O6S2.2ClH/c27-14-15-3-5-16(6-4-15)18-12-17-7-10-38-22(17)21(13-18)40(36,37)32-19-8-11-39-23(19)24(33)31-20(25(34)35)2-1-9-30-26(28)29;;/h3-6,8,11-13,20,32H,1-2,7,9-10,14,27H2,(H,31,33)(H,34,35)(H4,28,29,30);2*1H/t20-;;/m0../s1
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| Chemical Name |
(2S)-2-[[3-[[5-[4-(aminomethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid;dihydrochloride
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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 (e.g. under nitrogen), 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: 200 mg/mL (303.21 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (7.58 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 50.0 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: ≥ 5 mg/mL (7.58 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (7.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5161 mL | 7.5804 mL | 15.1607 mL | |
| 5 mM | 0.3032 mL | 1.5161 mL | 3.0321 mL | |
| 10 mM | 0.1516 mL | 0.7580 mL | 1.5161 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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