NaV1.7 inhibitor-1
Based on 1 Customer Validation
NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5.
For research use only. We do not sell to patients.
- Purity: 99.17%
- CAS No.: 1494585-79-3
- Formula: C23H30FNO4S
- Molecular Weight:435.55
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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h Nav1.7 0.6 nM (IC50) |
|
Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.002 μM
Compound: 12
|
Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay
|
[PMID: 31012583] |
| HEK293 | IC50 |
0.0022 μM
Compound: 12
|
Inhibition of mouse Nav1.7 expressed in HEK293 cells by electrophysiology assay
Inhibition of mouse Nav1.7 expressed in HEK293 cells by electrophysiology assay
|
[PMID: 31012583] |
| HEK293 | IC50 |
0.0037 μM
Compound: 12
|
Inhibition of rat Nav1.7 expressed in HEK293 cells by electrophysiology assay
Inhibition of rat Nav1.7 expressed in HEK293 cells by electrophysiology assay
|
[PMID: 31012583] |
| HEK293 | IC50 |
0.006 μM
Compound: 12
|
Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
|
[PMID: 31012583] |
| HEK293 | IC50 |
0.038 μM
Compound: 12
|
Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay
|
[PMID: 31012583] |
| HEK293 | IC50 |
0.05 μM
Compound: 12
|
Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
|
[PMID: 31012583] |
| HEK293 | IC50 |
0.0006 μM
Compound: 12
|
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
|
[PMID: 31012583] |
| HEK293 | IC50 |
0.6 nM
Compound: 12
|
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
|
[PMID: 31012583] |
Chemical Information
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CAS No. 1494585-79-3
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Appearance Solid
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Molecular Weight 435.55
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Formula C23H30FNO4S
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Color White to off-white
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SMILES
FC1=CC(OCC2(C)CCC3(CC3)CC2)=C(C4CC4)C=C1C(NS(C5CC5)(=O)=O)=O
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (229.59 mM; ultrasonic and warming and heat to 60°C; 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, 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.
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.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.74 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.
Please enter the basic information of animal experiments:
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-
-
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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 (271 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, 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 | 2.2959 mL | 11.4797 mL | 22.9595 mL | 57.3987 mL |
| 5 mM | 0.4592 mL | 2.2959 mL | 4.5919 mL | 11.4797 mL | |
| 10 mM | 0.2296 mL | 1.1480 mL | 2.2959 mL | 5.7399 mL | |
| 15 mM | 0.1531 mL | 0.7653 mL | 1.5306 mL | 3.8266 mL | |
| 20 mM | 0.1148 mL | 0.5740 mL | 1.1480 mL | 2.8699 mL | |
| 25 mM | 0.0918 mL | 0.4592 mL | 0.9184 mL | 2.2959 mL | |
| 30 mM | 0.0765 mL | 0.3827 mL | 0.7653 mL | 1.9133 mL | |
| 40 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4350 mL | |
| 50 mM | 0.0459 mL | 0.2296 mL | 0.4592 mL | 1.1480 mL | |
| 60 mM | 0.0383 mL | 0.1913 mL | 0.3827 mL | 0.9566 mL | |
| 80 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7175 mL | |
| 100 mM | 0.0230 mL | 0.1148 mL | 0.2296 mL | 0.5740 mL |