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

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.

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E0199

E0199 Chemical Structure

CAS No. : 931928-13-1

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Description

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)

In Vitro

E0199 (0.1-10 μM) influences the inactivation process of the NaV1.7, NaV1.8, and NaV1.9 channels, facilitating channel inactivation and impacting the extent of the shift of the inactive curve in the sequence: NaV1.8 > NaV1.9 > NaV1.7[1].
E0199 (0.03-10 μM) activates KV7.2-KV7.5 channels, moving their activation curve towards the hyperpolarisation direction and opening KV7 channels, demonstrating a rank order of potency of KV7.2/7.3 > KV7.2 > KV7.5 > KV7.4[1].
E0199 (1-10 μM) significantly influences action potential (AP) firing parameters in the CCI model rat Dorsal Root Ganglion (DRG) neurons in a dose-dependent manner, affecting the threshold, rheobase, amplitude, and Resting Membrane Potential (RMP)[1].

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

E0199 Related Antibodies
In Vivo

E0199 (1, 5, and 20 mg/kg, i.p., daily from day 11 to 30 after the induction of CCI) significantly alleviates thermal, mechanical, and cold hypersensitivity, enhances central open field movement, and improves exploratory behavior in the elevated plus maze in CCI mice[1].

MedChemExpress (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.
Molecular Weight

535.63

Formula

C29H37N5O5
CAS No.
SMILES

COC1=C(C=CC(CC(N2CCN(CC2)CC3=NOC(CCC(N(CC4=CC=CC=C4)CC)=O)=N3)=O)=C1)OC
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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E0199 Related Classifications

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  • 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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