| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
E0199 (0.1-10 μM) affects the inactivation process of NaV1.7, NaV1.8 and NaV1.9 sodium ion channels, promotes channel inactivation, and affects the degree of shift in the inactivation curve. The order is: NaV1.8 > NaV1.9 > NaV1.7[1]. E0199 (0.03-10 μM) can activate KV7.2 to KV7.5 potassium ion channels, causing their activation curves to shift towards hyperpolarization, thereby opening KV7 channels. The order of efficacy is KV7.2/7.3 > KV7.2 > KV7.5 > KV7.4[1]. E0199 (1-10 μM) significantly affects the firing parameters of action potentials (APs) of dorsal root ganglion (DRG) neurons in rats with chronic sciatic nerve compression injury (CCI) in a dose-dependent manner, including threshold, base strength, amplitude and resting membrane potential (RMP)[1].
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|---|---|
| ln Vivo |
E0199 (1, 5 and 20 mg/kg, intraperitoneal injection, once daily, from day 11 to 30 after modeling) significantly alleviated thermal, mechanical and cold hypersensitivity responses, increased central open field movement, and improved exploratory behavior in the elevated cruciate maze in a model of chronic sciatic nerve injury (CCI) [1].
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| Animal Protocol |
Animal/Disease Models: Male C57 mice (8-10 weeks old) with CCI under isoflurane anesthesia[1]
Doses: 1, 5, and 20 mg/kg Route of Administration: i.p., daily from day 11 to 30 after the induction of CCI Experimental Results: 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. |
| References |
| Molecular Formula |
C29H37N5O5
|
|---|---|
| Molecular Weight |
535.63
|
| CAS # |
931928-13-1
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| Appearance |
Typically exists as solids at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1867 mL | 0.9335 mL | 1.8670 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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