Nav1.1 activator 1
Based on 1 Customer Validation
Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.
For research use only. We do not sell to patients.
- Purity: 98.98%
- CAS No.: 2332897-85-3
- Formula: C24H23F3N4O
- Molecular Weight:440.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Nav1.1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1].
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Dosage:30 mg/kg (Pharmacokinetic Analysis).
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Administration:IP once (Exposure was measured at 1 h after administration).
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Result:Intraperitoneal administration (30 mg/kg) of compound resulted in sufficient brain exposure (193 ng/g 1 h after administration), which corresponded to 13 nM of free brain concentration comparable to the in vitro potency of the compound.
Had a potential use as an in vivo tool to investigate whether this type of Nav1.1 activator can restore Nav1.1 functions and modify the disease state in animal models.
Could penetrate the blood-brain barrier (BBB) in humans.
Chemical Information
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CAS No. 2332897-85-3
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Appearance Solid
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Molecular Weight 440.46
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Formula C24H23F3N4O
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Color White to off-white
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SMILES
O=C(C1=C(C2=CC(F)=CC=C2F)C=CN=C1N3C[C@@H](F)CC3)NC4=CC=C(C(C)C)N=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 : 250 mg/mL (567.59 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.72 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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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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 (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 |
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| DMSO | 1 mM | 2.2704 mL | 11.3518 mL | 22.7035 mL | 56.7588 mL |
| 5 mM | 0.4541 mL | 2.2704 mL | 4.5407 mL | 11.3518 mL | |
| 10 mM | 0.2270 mL | 1.1352 mL | 2.2704 mL | 5.6759 mL | |
| 15 mM | 0.1514 mL | 0.7568 mL | 1.5136 mL | 3.7839 mL | |
| 20 mM | 0.1135 mL | 0.5676 mL | 1.1352 mL | 2.8379 mL | |
| 25 mM | 0.0908 mL | 0.4541 mL | 0.9081 mL | 2.2704 mL | |
| 30 mM | 0.0757 mL | 0.3784 mL | 0.7568 mL | 1.8920 mL | |
| 40 mM | 0.0568 mL | 0.2838 mL | 0.5676 mL | 1.4190 mL | |
| 50 mM | 0.0454 mL | 0.2270 mL | 0.4541 mL | 1.1352 mL | |
| 60 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9460 mL | |
| 80 mM | 0.0284 mL | 0.1419 mL | 0.2838 mL | 0.7095 mL | |
| 100 mM | 0.0227 mL | 0.1135 mL | 0.2270 mL | 0.5676 mL |
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