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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C29H36N10O7S3
- 分子量:732.85
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
VEGFR アイソフォーム固有の製品をすべて表示
More
生物活性
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.
-
Cell Line:Vascular endothelial cells of the ex vivo mouse retina and Human brain endothelial line hCMEC/D3
-
Concentration:30 μM
-
Incubation Time:Preincubated for 15 min and then treated with VEGFA for 5 min.
-
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.
-
Animal Model:Male and female rats (6 weeks old) were given an intraplantar injection in the hind-paw containing VEGFA165 (10 nM)[1]
-
Dosage:10 μM, 30 μM
-
Administration:Intraplantar injection; once
-
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.
-
Animal Model:Male and female rats (6 weeks old) were given an intraplantar injection in the hind-paw containing VEGFA165 (10 nM)[1]
-
Dosage:10 μM, 30 μM
-
Administration:Intraplantar injection; once
-
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.
化学情報
-
分子量 732.85
-
分子式 C29H36N10O7S3
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
EG01449 関連分類
HY-179350A 関連分類
Powered by Bioz