EG01449
EG01449 is a quinoline-based antagonist of Neuropilin-1 (NRP1) with an Kd of 0.6 µM. EG01449 competitively inhibits the binding of VEGFA to NRP1 with an IC50 of 362 nM. EG01449 prevents VEGFA-induced pain by inhibiting NRP1-dependent signaling and reducing sodium currents in sensory neurons. EG01449 can be used for the research of nociceptive pain.
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- Formule: C29H36N10O7S3
- Masse moléculaire:732.85
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
EG01449 (30 μM; Preincubation for 15 min) reduces VEGFA-induced phosphorylation of p38 in retinal endothelium and hCMEC/D3[1].
EG01449 (30 μM; Excised Rat Lumbar DRG Neurons) reduces VEGFA165-induced increase in sodium currents. EG01449 alone has any obvious effect on Na+ currents[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Vascular endothelial cells of the ex vivo mouse retina and Human brain endothelial line hCMEC/D3
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Concentration:30 μM
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Incubation Time:Preincubated for 15 min and then treated with VEGFA for 5 min.
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Result:VEGFA-induced phosphorylation of p38 phosphorylation was inhibited.
| Species | Dose | Route | Note | AUC | Plasma Concentration | Clearance (CL) | T1/2 | Tmax | Cmax | Vd |
|---|---|---|---|---|---|---|---|---|---|---|
| Mice | 2 mg/kg | i.v. | 文献审核 | 1367 ng·h/mL | 5181 ng/mL | 24.33 mL/min/kg | 1.3 h | 0.08 h | 5181 ng/mL | 394 mL/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male and female rats (6 weeks old) were given an intraplantar injection in the hind-paw containing VEGFA165 (10 nM)[1]
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Dosage:10 μM, 30 μM
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Administration:Intraplantar injection; once
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Result:Significantly reduced VEGFA-induced mechanical allodynia in both male and female rats at 30 μM. At 10 μM, significant reduction in mechanical allodynia in males but not in females. Additionally, significantly reduced VEGFA-induced cold allodynia in females at 30 μM, but not at 10 μM. No significant effects were observed in females at 10 μM.
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Animal Model:Male and female rats (6 weeks old) were given an intraplantar injection in the hind-paw containing VEGFA165 (10 nM)[1]
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Dosage:10 μM, 30 μM
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Administration:Intraplantar injection; once
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Result:Significantly reduced VEGFA-induced aversion to mechanical stimuli in both male and female rats at 30 μM. At 10 μM, significant reduction in aversion in males but not in females. No significant effects were observed in females at 10 μM.
Chemical Information
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Masse moléculaire 732.85
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Formule C29H36N10O7S3
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SMILES
O=C([C@H](CCCNC(N)=N)NC(C1=C(C=CS1)NS(=O)(C2=C3N=CC=CC3=CC(NCC4=CSC(N5CCNCC5)=N4)=C2)=O)=O)O.O=CO
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EG01449 Related Classifications
HY-179350A Related Classifications
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