Sodium Channel inhibitor 1
Based on 1 Customer Validation
Sodium Channel inhibitor 1 is a state-dependent voltage-gated NaV1.7 inhibitor with an IC50 of 0.087 μM. Sodium Channel inhibitor 1 can be used for research of pain.
For research use only. We do not sell to patients.
- Purity: 99.38%
- CAS No.: 1198117-23-5
- Formula: C24H19F4N3O3
- Molecular Weight:473.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
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Nav1.7 0.087 μM (IC50) |
hNav1.5 0.81 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
0.81 μM
Compound: 53
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Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assay
Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assay
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[PMID: 22770500] |
| CHO-K1 | IC50 |
5.6 μM
Compound: 53
|
Binding affinity to human ERG expressed in CHOK1 cells by IonWorks HT assay
Binding affinity to human ERG expressed in CHOK1 cells by IonWorks HT assay
|
[PMID: 22770500] |
| HEK293 | IC50 |
0.087 μM
Compound: 53
|
Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay
Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay
|
[PMID: 22770500] |
| HEK293 | IC50 |
0.28 μM
Compound: 53
|
Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -90 mV holding potential by patch clamp electrophysiological assay
Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -90 mV holding potential by patch clamp electrophysiological assay
|
[PMID: 22770500] |
Sodium Channel inhibitor 1 (compund 53) shows moderate selectivity over human NaV1.5 (IC50 = 0.81 μM), along with measurable hERG inhibition (IC50 = 5.6 μM), moderate solubility, and moderate metabolic stability in rat and human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1198117-23-5
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Appearance Solid
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Molecular Weight 473.42
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Formula C24H19F4N3O3
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Color White to off-white
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SMILES
O=C(C1N(CCC2=NC=CC=C2)C(C3=C1C(F)=CC=C3)=O)NCC4=CC=C(OC(F)(F)F)C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 100 mg/mL (211.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1123 mL | 10.5614 mL | 21.1229 mL | 52.8072 mL |
| 5 mM | 0.4225 mL | 2.1123 mL | 4.2246 mL | 10.5614 mL | |
| 10 mM | 0.2112 mL | 1.0561 mL | 2.1123 mL | 5.2807 mL | |
| 15 mM | 0.1408 mL | 0.7041 mL | 1.4082 mL | 3.5205 mL | |
| 20 mM | 0.1056 mL | 0.5281 mL | 1.0561 mL | 2.6404 mL | |
| 25 mM | 0.0845 mL | 0.4225 mL | 0.8449 mL | 2.1123 mL | |
| 30 mM | 0.0704 mL | 0.3520 mL | 0.7041 mL | 1.7602 mL | |
| 40 mM | 0.0528 mL | 0.2640 mL | 0.5281 mL | 1.3202 mL | |
| 50 mM | 0.0422 mL | 0.2112 mL | 0.4225 mL | 1.0561 mL | |
| 60 mM | 0.0352 mL | 0.1760 mL | 0.3520 mL | 0.8801 mL | |
| 80 mM | 0.0264 mL | 0.1320 mL | 0.2640 mL | 0.6601 mL | |
| 100 mM | 0.0211 mL | 0.1056 mL | 0.2112 mL | 0.5281 mL |