1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. Benzocaine

Benzocaine 

Cat. No.: HY-Y0258 Purity: 99.98%
Handling Instructions

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.

For research use only. We do not sell to patients.

Benzocaine Chemical Structure

Benzocaine Chemical Structure

CAS No. : 94-09-7

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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
500 mg USD 50 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

Clinical Trial
Molecular Weight

165.19

Formula

C₉H₁₁NO₂

CAS No.

94-09-7

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)

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
10 mM 0.6054 mL 3.0268 mL 6.0536 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (15.13 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

BenzocaineSodium ChannelNa channelsNa+ channelsInhibitorinhibitorinhibit

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Benzocaine
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HY-Y0258
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