2. Membrane Transporter/Ion Channel
  3. Potassium Channel Sodium Channel
  4. E0199

E0199 是一种新型有效的 KV7/NaV 双靶点调节剂，它能够激活 KV7 钾离子通道 (包括 (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), 和 KV7.5 (EC50 = 27.14 nM))，同时抑制 NaV1.7 (IC50 = 0.52 μM)、NaV1.8 (IC50 = 0.24 μM) 和 NaV1.9 (IC50 = 0.16 μM) 钠离子通道。在慢性坐骨神经压迫损伤 (CCI) 小鼠模型中，E0199 显示出强效的镇痛作用，且对心脏和骨骼肌离子通道无严重影响。E0199 可用于神经病理性疼痛 (NP) 的相关研究。

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E0199

E0199 Chemical Structure

CAS No. : 931928-13-1

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E0199 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

E0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research[1].

IC50 & Target[1]

Nav1.7

0.52 μM (IC50)

Nav1.8

0.24 μM (IC50)

Nav1.9

0.16 μM (IC50)

体外研究
(In Vitro)

E0199 (0.1-10 μM) 影响 NaV1.7、NaV1.8 和 NaV1.9 钠离子通道的失活过程，促进通道失活，并影响失活曲线的偏移程度，其顺序为： NaV1.8 > NaV1.9 > NaV1.7[1]。
E0199 (0.03-10 μM) 可激活 KV7.2 至 KV7.5 钾离子通道，使其激活曲线向超极化方向移动，从而打开 K 7 通道，其效力顺序为 KV7.2/7.3 > KV7.2 > KV7.5 > KV7.4[1]。
E0199 (1-10 μM) 以剂量依赖性方式显著影响坐骨神经慢性压迫损伤 (CCI) 模型大鼠背根神经节 (DRG) 神经元的动作电位 (AP) 的放电参数，包括阈值、基强度、振幅和静息膜电位 (RMP)[1]。

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

E0199 相关抗体:
体内研究
(In Vivo)

E0199 (1、5 和 20 mg/kg，腹腔注射，每日一次，造模后第 11 至 30 天) 在坐骨神经慢性压迫性损伤 (CCI) 小鼠模型中，能显著缓解其热、机械和冷超敏反应，增加旷场中央区运动，并改善其在高架十字迷宫中的探索行为[1]。

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

Animal Model: Male C57 mice (8-10 weeks old) with CCI under isoflurane anesthesia[1]
Dosage: 1, 5, and 20 mg/kg
Administration: i.p., daily from day 11 to 30 after the induction of CCI
Result: Significantly alleviated thermal, mechanical, and cold hypersensitivity in CCI mice with effects observed across all dose levels.
Maintained significantly higher thermal and mechanical withdrawal thresholds than the model group even on day 15 at 5 mg/kg.
Showed a significant increase in the mechanical withdrawal threshold on day 15 at 1 mg/kg.
Maintained higher cold withdrawal thresholds than other groups at 5 and 20 mg/kg.
Prolonged the time and the distance of movement in the central open field.
Enhanced the total distance and average speed, and improved exploratory ability in the elevated plus maze.
Increased movement time in the open arms and central zone compared to the model group, with no significant difference between the blank and sham surgery groups at 20 mg/kg.
Significantly reduced the proportion of movement time spent in the dark arms from 88.37 % to 67.51 % and 61.68 %, at 5 and 20 mg/kg, respectively.
分子量

535.63

Formula

C29H37N5O5
CAS 号
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

E0199 相关分类

  • 摩尔计算器

  • 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:

E0199931928-13-1E 0199E-0199Potassium ChannelSodium ChannelKcsANa channelsNa+ channelsKV7/NaVanalgesicCCINPNaV1.7NaV1.8NaV1.9KV7KV7.2/7.3KV7.2KV7.5Inhibitorinhibitorinhibit

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目录号：
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