E0199 |
Katalog-Nr.GC79544
One-Click Copy Product Info
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E0199 is a novel potent dual-target K V 7/Na V modulator that activates the K V 7 channel (K V 7.2/7.3 ( EC 50 = 12.78 nM), K V 7.2 ( EC 50 = 0.50 μM), and K V 7.5 ( EC 50 = 27.14 nM) channels) while simultaneously blocks the Na V 1.7 ( IC50 = 0.52 μM), Na V 1.8 ( IC50 = 0.24 μM), and Na V 1.9 ( IC50 = 0.16 μM) channels.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 931928-13-1
Sample solution is provided at 25 µL, 10mM.
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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].
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].
References:
[1]. Zhang B, et al. Discovery of E0199: A novel compound targeting both peripheral NaV and KV7 channels to alleviate neuropathic pain. J Pharm Anal. 2025 Jan;15(1):101132.
| Cas No. | 931928-13-1 | SDF | |
| Formula | C29H37N5O5 | M.Wt | 535.63 |
| Löslichkeit | DMSO: 50 mg/mL (93.35 mM; Need ultrasonic) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.867 mL | 9.3348 mL | 18.6696 mL |
| 5 mM | 373.4 μL | 1.867 mL | 3.7339 mL |
| 10 mM | 186.7 μL | 933.5 μL | 1.867 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: An oil
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)