EG00229 |
| Catalog No.GC16183 |
Nrp1 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1210945-69-9
Sample solution is provided at 25 µL, 10mM.
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EG00229 is a small molecule inhibitor of neuropilin-1(Nrp1) with an IC50 of 3μM [1].
EG00229 has been reported to inhibit VEGF-A binding to PAE/NRP1 in the Nrp1and bt-VEGF-A binding to purified Nrp1 b1 domain in a cell-free assay with an IC50 value of 8μM and 3μM, respectively. In addition, EG00229 has also shown the inhibition of VEGF-A binding to VEGFR2, VEGFR1 and Nrp1 in human umbilical vein endothelial cells (HUVECs) in a dose-dependent manner with an IC50 value of 23μM [1]. Besides, EG00229 has been revealed to prevent tuftsin binding to the Nrp1 which is at the cell surface. Moreover, EG00229 has been noted to suppress the anti-inflammatory M2 shift in microglia induced by tuftsin and thus potently prevent tuftsin’s action [2].
References:
[1] Jarvis A1, Allerston CK, Jia H, Herzog B, Garza-Garcia A, Winfield N, Ellard K, Aqil R, Lynch R, Chapman C, Hartzoulakis B, Nally J, Stewart M, Cheng L, Menon M, Tickner M, Djordjevic S, Driscoll PC, Zachary I, Selwood DL.Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction. J Med Chem. 2010 Mar 11;53(5):2215-26.
[2] Nissen JC1, Selwood DL, Tsirka SE. Tuftsin signals through its receptor neuropilin-1 via the transforming growth factor beta pathway. J Neurochem. 2013 Nov;127(3):394-402.
| Cas No. | 1210945-69-9 | SDF | |
| Chemical Name | (S,Z)-2-(((3-(benzo[c][1,2,5]thiadiazole-4-sulfonamido)thiophen-2-yl)(hydroxy)methylene)amino)-5-guanidinopentanoic acid compound with 2,2,2-trifluoroacetic acid (1:1) | ||
| Canonical SMILES | N=C(NCCC[C@@](/N=C(O)/C1=C(NS(C2=CC=CC3=NSN=C32)(=O)=O)C=CS1)([H])C(O)=O)N.FC(F)(F)C(O)=O | ||
| Formula | C19H20F3N7O7S3 | M.Wt | 611.6 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6351 mL | 8.1753 mL | 16.3506 mL |
| 5 mM | 0.327 mL | 1.6351 mL | 3.2701 mL |
| 10 mM | 0.1635 mL | 0.8175 mL | 1.6351 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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