Benzonatate
Based on 1 Customer Validation
Benzonatate (Benzononatine) is an orally active and non-narcotic peripheral antitussive agent. Benzonatate is a reversible voltage-gated Na+ channels inhibitor. Benzonatate dampens the activity of cough stretch receptors.
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- Pureza: 98.96%
- No. CAS: 104-31-4
- Fòrmula: C30H53NO11
- Peso molecular:603.74
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Benzonatate mechanism of action is through its peripheral anesthetic dampening the activity of pulmonary stretch receptors located in respiratory passages, lungs, and pleura, which mediate the cough reflex). It also has similar activity on aortic baroreceptors, atrial and vagal receptors. Benzonatate has no inhibitory action in the respiratory center[1].
In two murine cell lines, catecholamine A differentiated (CAD) cells, which express primarily Nav1.7, and N1E-115, which express primarily Nav1.3, Benzonatate strongly and reversibly inhibits voltage-gated Na+ channels. Benzonatate causes both tonic and phasic inhibition in CAD cells and N1E-115 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 104-31-4
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Appearance Liquid (Density: 1.096 g/cm3)
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Peso molecular 603.74
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Fòrmula C30H53NO11
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Color Colorless to light yellow
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SMILES
O=C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOC)C1=CC=C(NCCCC)C=C1
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Synonyms
Benzononatine
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (165.63 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, 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.14 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 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: ≥ 2.5 mg/mL (4.14 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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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.
Pureza y Documentación
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Ficha de datos (267 KB)
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SDS (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 1.6563 mL | 8.2817 mL | 16.5634 mL | 41.4086 mL |
| 5 mM | 0.3313 mL | 1.6563 mL | 3.3127 mL | 8.2817 mL | |
| 10 mM | 0.1656 mL | 0.8282 mL | 1.6563 mL | 4.1409 mL | |
| 15 mM | 0.1104 mL | 0.5521 mL | 1.1042 mL | 2.7606 mL | |
| 20 mM | 0.0828 mL | 0.4141 mL | 0.8282 mL | 2.0704 mL | |
| 25 mM | 0.0663 mL | 0.3313 mL | 0.6625 mL | 1.6563 mL | |
| 30 mM | 0.0552 mL | 0.2761 mL | 0.5521 mL | 1.3803 mL | |
| 40 mM | 0.0414 mL | 0.2070 mL | 0.4141 mL | 1.0352 mL | |
| 50 mM | 0.0331 mL | 0.1656 mL | 0.3313 mL | 0.8282 mL | |
| 60 mM | 0.0276 mL | 0.1380 mL | 0.2761 mL | 0.6901 mL | |
| 80 mM | 0.0207 mL | 0.1035 mL | 0.2070 mL | 0.5176 mL | |
| 100 mM | 0.0166 mL | 0.0828 mL | 0.1656 mL | 0.4141 mL |
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