2. Membrane Transporter/Ion Channel Anti-infection
  3. Sodium Channel Bacterial
  4. Benzocaine

Benzocaine shares a common receptor with all othe rLAs in the voltage-gated Na+ channel, with an IC50 of 0.8 mM tested with a potential of +30 mV.

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Benzocaine Chemical Structure

Benzocaine Chemical Structure

CAS No. : 94-09-7

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Benzocaine:

Benzocaine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Benzocaine

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Benzocaine shares a common receptor with all othe rLAs in the voltage-gated Na+ channel, with an IC50 of 0.8 mM tested with a potential of +30 mV.

IC50 & Target

IC50: 0.8 mM (Na+ channel)[1].
In Vitro

Benzocaine blocks μ1 wild-type Na+ currents in a dose-dependent Manner. The Benzocaine concentration that inhibits 50% of Na+ currents (IC50) is estimated to be about 0.8 mM when a test potential of +30 mV is applied. The slope of the h∞ curve is also significantly reduced by benzocaine (from 6.6 to 9.9 mV). Mutation of μ1-N1584A also significantly increases the potency of Benzocaine. At 1 mM, Benzocaine blocks about 55% of wild-type Na+ current but about 95% of μ1-N1584A mutant current. Benzocaine also appears to bind more strongly to its LA receptor in the N1584A mutant than in the wild type[1]. The inhibition of Ca2+ uptake occurres at lower Benzocaine concentration (IC50=40.3±1.2mM) than that affecting the enzymatic activity[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Benzocaine Related Antibodies
In Vivo

Benzocaine is topically applied to the following species: dogs, domestic shorthair cats, Long-Evans rats, Sprague-Dawley rats, ferrets, rhesus monkeys, cynomolgus monkeys, owl monkeys, New Zealand White rabbits, miniature pigs, ICR mice, C3H mice, and C57BL/10SnJ mice. All animals, except mice and rats, receive a 2-second spray to the mucous membranes of the nasopharynx for an estimated dose of 56 mg. A 2-second spray to rodents' oral mucous membranes delivers too great a volume of fluid for these animals. The study is repeated in dogs several months later to confirm low response. Response to Benzocaine spray is observed in most animals tested, with response peaking between 15 and 30 minutes after dosing[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

165.19

Formula

C9H11NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OCC)C1=CC=C(N)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (605.36 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 2 mg/mL (12.11 mM; ultrasonic and warming and heat to 60°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 6.0536 mL 30.2682 mL 60.5364 mL
5 mM 1.2107 mL 6.0536 mL 12.1073 mL
View the 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (15.13 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (15.13 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.96%

COA (244 KB) RP-HPLC (244 KB)

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 (protect from light). 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
H2O / DMSO 1 mM 6.0536 mL 30.2682 mL 60.5364 mL 151.3409 mL
5 mM 1.2107 mL 6.0536 mL 12.1073 mL 30.2682 mL
10 mM 0.6054 mL 3.0268 mL 6.0536 mL 15.1341 mL
DMSO 15 mM 0.4036 mL 2.0179 mL 4.0358 mL 10.0894 mL
20 mM 0.3027 mL 1.5134 mL 3.0268 mL 7.5670 mL
25 mM 0.2421 mL 1.2107 mL 2.4215 mL 6.0536 mL
30 mM 0.2018 mL 1.0089 mL 2.0179 mL 5.0447 mL
40 mM 0.1513 mL 0.7567 mL 1.5134 mL 3.7835 mL
50 mM 0.1211 mL 0.6054 mL 1.2107 mL 3.0268 mL
60 mM 0.1009 mL 0.5045 mL 1.0089 mL 2.5223 mL
80 mM 0.0757 mL 0.3784 mL 0.7567 mL 1.8918 mL
100 mM 0.0605 mL 0.3027 mL 0.6054 mL 1.5134 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Benzocaine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Benzocaine94-09-7Sodium ChannelBacterialNa channelsNa+ channelsInhibitorinhibitorinhibit

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