| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
Benzocaine hydrochloride targets voltage-gated sodium (Na+) channels on nerve membranes. It binds reversibly to a common receptor site in the channel pore, inhibiting sodium influx. This prevents the generation and propagation of action potentials, thereby blocking sensory impulse transmission and producing local anesthesia.
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|---|---|
| ln Vitro |
In vitro, benzocaine hydrochloride blocks voltage-gated Na+ channels (IC₅0 = 0.8 mM at +30 mV). It is used in patch-clamp electrophysiology (0.1-10 mM) to study Na+ channel pharmacology. It is also moderately cytotoxic to fibroblasts at >5 mM, but is safe at topical anesthetic concentrations (1-5%).
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| ln Vivo |
In vivo, benzocaine hydrochloride is an orally active topical anesthetic. Topical application to mucous membranes (oral, pharyngeal) provides rapid-onset (30-60 seconds), short-acting (10-30 minutes) relief. It is absorbed systemically only in very small amounts, minimizing systemic toxicity. It is also used in dental procedures to anesthetize gingival tissues.
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| Enzyme Assay |
For Na+ channel assays, HEK293 cells expressing hNav1.7 are whole-cell patch-clamped, and the compound is applied at concentrations of 0.1-10 mM. Inhibition is measured as % decrease in peak sodium current from a holding potential of -80 mV to a test potential of 0 mV.
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| Cell Assay |
For viability assays, cells are seeded in 96-well plates (1 × 10⁴ cells/well) and treated with 0.1-10 mM benzocaine hydrochloride for 24-48 h. Viability is assessed by MTT; IC₅0 >5 mM. For skin irritation tests, 3D skin models (EpiDerm) are treated topically with 5% benzocaine hydrochloride and assessed for IL-1alpha release.
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| Animal Protocol |
For dermal anesthesia, guinea pigs are depilated, and benzocaine hydrochloride gel (5-20%) is applied to the skin for 30 min. Pinprick testing assesses analgesia. For oral anesthesia, dogs are sedated, the gel is applied to the gingiva, and electrodontal testing is performed.
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| ADME/Pharmacokinetics |
Benzocaine hydrochloride is water-soluble (40 mg/mL in DMSO) but is primarily used topically. Applied to mucous membranes, systemic absorption is low (<10%). It is rapidly hydrolyzed by plasma pseudocholinesterase to para-aminobenzoic acid (PABA) and ethanol, which are excreted in urine.
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| Toxicity/Toxicokinetics |
Benzocaine hydrochloride has low acute toxicity (LD₅0 oral > 3000 mg/kg in rats). Topical use may cause hypersensitivity reactions (contact dermatitis) due to PABA. Methemoglobinemia is a rare but serious adverse effect. It is not genotoxic or carcinogenic.
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| References |
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| Additional Infomation |
See also: Lidocaine Hydrochloride (related); Benzocaine (has active moiety).
Benzocaine hydrochloride is an FDA-approved (OTC) local anesthetic. It is a standard agent for topical pain relief and is included in numerous OTC products. It is not for injection and is not used systemically. Its use is limited by the potential for methemoglobinemia, especially in infants. |
| Molecular Formula |
C9H12CLNO2
|
|---|---|
| Molecular Weight |
201.65
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| Exact Mass |
201.056
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| CAS # |
23239-88-5
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| Related CAS # |
94-09-7 (Parent)
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| PubChem CID |
10214462
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| Appearance |
White to off-white solid powder
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| Density |
1.286g/cm3
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| Boiling Point |
495ºC at 760mmHg
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| Melting Point |
208ºC
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| Flash Point |
228.6ºC
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| Vapour Pressure |
0.000589mmHg at 25°C
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| LogP |
2.829
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
13
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| Complexity |
151
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(OCC)C1=CC=C(N)C=C1.[H]Cl
|
| InChi Key |
JAADDQHUJDUAKW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H11NO2.ClH/c1-2-12-9(11)7-3-5-8(10)6-4-7;/h3-6H,2,10H2,1H3;1H
|
| Chemical Name |
ethyl 4-aminobenzoate;hydrochloride
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| Synonyms |
Benzocaine base
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9591 mL | 24.7954 mL | 49.5909 mL | |
| 5 mM | 0.9918 mL | 4.9591 mL | 9.9182 mL | |
| 10 mM | 0.4959 mL | 2.4795 mL | 4.9591 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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