2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. EG01449

EG01449 是一种喹啉类神经纤毛蛋白-1 (NRP1) 拮抗剂，其 Kd 值为 0.6 µM。EG01449 可竞争性抑制 VEGFA 与 NRP1 的结合，IC50 值为 362 nM。EG01449 通过抑制 NRP1-依赖性信号传导和减少感觉神经元中的钠电流，防止 VEGFA 引起的疼痛。EG01449 可以穿过血脑屏障，使中枢神经系统内可以进行靶向作用。EG01449 可用于研究疼痛。

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EG01449

EG01449 Chemical Structure

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EG01449 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

体外研究
(In Vitro)

EG01449 (30 μM；预处理 15 分钟) 降低 VEGFA 诱导的视网膜内皮和 hCMEC/D3 中 p38 的磷酸化[1]。
EG01449 (30 μM；离体的大鼠腰椎 DRG 神经元) 减少 VEGFA165 引起的钠电流增加。单独使用 EG01449 未对 Na+ 电流产生明显影响[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

EG01449 相关抗体:

Western Blot Analysis[1]

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.
体内研究
(In Vivo)

EG01449 (10, 30 μM；足底注射；单次注射) 在 Sprague-Dawley 大鼠中显著降低 VEGFA 引起的对机械刺激的厌恶和 VEGFA 引起的机械性和冷性痛觉过敏[1]。

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.
分子量

732.85

Formula

C29H36N10O7S3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

EG01449 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EG01449EG 01449EG-01449VEGFRVascular endothelial growth factor receptorneuropilin antinociceptive chronic pain VEGF NRP1Inhibitorinhibitorinhibit

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产品名称：
EG01449
目录号：
HY-179350A
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