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

Size Price Stock Quantity
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

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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.
Appearance

Oil

Color

Colorless to light yellow

SMILES

COC1=C(C=CC(CC(N2CCN(CC2)CC3=NOC(CCC(N(CC4=CC=CC=C4)CC)=O)=N3)=O)=C1)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (93.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8670 mL 9.3348 mL 18.6696 mL
5 mM 0.3734 mL 1.8670 mL 3.7339 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.89%

SDS (252 KB)

COA (248 KB) HNMR (141 KB) LCMS (332 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8670 mL 9.3348 mL 18.6696 mL 46.6740 mL
5 mM 0.3734 mL 1.8670 mL 3.7339 mL 9.3348 mL
10 mM 0.1867 mL 0.9335 mL 1.8670 mL 4.6674 mL
15 mM 0.1245 mL 0.6223 mL 1.2446 mL 3.1116 mL
20 mM 0.0933 mL 0.4667 mL 0.9335 mL 2.3337 mL
25 mM 0.0747 mL 0.3734 mL 0.7468 mL 1.8670 mL
30 mM 0.0622 mL 0.3112 mL 0.6223 mL 1.5558 mL
40 mM 0.0467 mL 0.2334 mL 0.4667 mL 1.1669 mL
50 mM 0.0373 mL 0.1867 mL 0.3734 mL 0.9335 mL
60 mM 0.0311 mL 0.1556 mL 0.3112 mL 0.7779 mL
80 mM 0.0233 mL 0.1167 mL 0.2334 mL 0.5834 mL
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E0199 Related Classifications

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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