Benzonatate |
|
カタログ番号GC42919
|
ベンゾナテート(ベンゾノナチン)は、咳ストレッチ受容体の活性を弱める末梢経口鎮咳薬です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 104-31-4
Sample solution is provided at 25 µL, 10mM.
Benzonatate, a long chain polyglycol derivative chemically related to procaine, is a peripherally-acting and oral antitussive [1]. The antitussive effect of benzonatate is achieved by inhibiting the pulmonary stretch receptors, and it is realized through reversible and concentration-dependent inhibition of voltage-gated sodium channels (including Nav1.7) [2]. Benzonatate has been used to prevent the initiation and propagation of action potentials in the nerves responsible for detecting and responding to irritants in the airways [3].
In vivo, Benzonatate was injected at the sciatic nerve of Sprague-Dawley rats at a dose of 0.3ml (12.4mM) for 4 days, which induced sensory and motor blockage and caused inflammation and myotoxicity[4].
References:
[1] Dicpinigaitis P V, Gayle Y E, Solomon G, et al. Inhibition of cough-reflex sensitivity by benzonatate and guaifenesin in acute viral cough[J]. Respiratory medicine, 2009, 103(6): 902-906.
[2] Evans M S, Maglinger G B, Fletcher A M, et al. Benzonatate inhibition of voltage-gated sodium currents[J]. Neuropharmacology, 2016, 101: 179-187.
[3] Foti Randazzese S, Toscano F, Gambadauro A, et al. Neuromodulators in acute and chronic cough in children: an update from the literature[J]. International Journal of Molecular Sciences, 2024, 25(20): 11229.
[4] McGuire A, Ostertag-Hill C A, Aizik G, et al. Benzonatate as a local anesthetic[J]. PLoS One, 2023, 18(4): e0284401.
| Animal experiment [1]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Sprague-Dawley rats were single housed in a temperature-controlled room with a 12:12h light-dark cycle and allowed ad libitum access to water and food. Rats were anesthetized using isoflurane. A 23-gauge needle was introduced posteromedial to the greater trochanter, and upon contact with the bone, 0.3ml of Benzonatate (12.4mM) was injected, depositing the injectate over the sciatic nerve. Rats were euthanized with carbon dioxide four days after injection, the time point at which local anesthetic inflammation and toxicity is expected. The sciatic nerve and surrounding tissues were harvested, fixed in 10% neutral buffered formalin, embedded in paraffin, sectioned, and stained with hematoxylin and eosin using standard techniques. |
Dosage form | 0.3ml (12.4mM) for once; sciatic nerve injection |
Applications | Benzonatate treatment caused inflammation and myotoxicity in sciatic nerve and surrounding tissues of rats. |
References: | |
| Cas No. | 104-31-4 | SDF | |
| Chemical Name | 4-(butylamino)-benzoic acid, 3,6,9,12,15,18,21,24,27-nonaoxaoctacos-1-yl ester | ||
| Canonical SMILES | O=C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOC)C1=CC=C(NCCCC)C=C1 | ||
| Formula | C30H53NO11 | M.Wt | 603.8 |
| 溶解度 | DMF: 50 mg/ml,DMSO: 50 mg/ml,Ethanol: 50 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6562 mL | 8.2809 mL | 16.5618 mL |
| 5 mM | 331.2 μL | 1.6562 mL | 3.3124 mL |
| 10 mM | 165.6 μL | 828.1 μL | 1.6562 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solution in ethanol
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)















