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Benzocaine

Catalog No. T0924 CAS 94-09-7

Benzocaine is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.

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Benzocaine, CAS 94-09-7

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500 mg	In stock	$ 42.00
1 mL * 10 mM (in DMSO)	In stock	$ 46.00

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Purity: 99.97%

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Description	Benzocaine is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.
Targets&IC50	Na+ channel:0.8 mM (IC50)
In vitro	Benzocaine blocks μ1 wild-type Na+ currents in a dose-dependent manner with IC50 of 0.8 mM in HEK293T cells. Benzocaine (1 mM) blocks about 55% of wild-type Na+ current but about 95% of μ1-N1584A mutant current. Benzocaine (1 mM) blocks about 55% of wild-type μ1 currents, but about 80% of μ1-I1575A mutant current. [1] Benzocaine results in a biphasic (protective/inductive) concentration-dependent hemolytic effect upon rat erythrocytes, with an effective Benzocaine:lipid molar ratio in the membrane for protection (RePROT), onset of hemolysis (ReSAT) and 100% membrane solubilization (ReSOL) of 1.0:1, 1.1:1 and 1.3:1, respectively. [2] Benzocaine and 4-hydroxybenzoate interact with the open and inactivated channels during repetitive pulses, but during the interpulse the complex dissociates too fast to accumulate sufficient use-dependent block of Na+ currents. [3] Benzocaine (500 μM) reduces the peak and steady-state currents and increases the amplitude of the inactivating component from 21.7% to 30.2% (n=7, P<0.05), so that benzocaine-induced block at the end of pulses to +60 mV averaged 30.9% (n=7). Benzocaine (500 μM) significantly accelerates the initial phase of deactivation (τf=27.2±2.6 ms, n=7, P<0.01), but does not modify the slow phase of tail current decline. Benzocaine binds with high affinity to an intracellular binding site to produce 'agonist' effects and to a low affinity subsite, which is also located in the inner mouth, to produce the blocking effects. Benzocaine and extracellular K(+) interact to modify the voltage-dependence of channel opening. [4]
In vivo	Benzocaine is absorbed rapidly and similarly through both viable and nonviable skin of the hairless guinea pig, the absorption of the two acidic compounds, benzoic acid and PABA, is greater through nonviable skin. [5]

Molecular Weight	165.19
Formula	C9H11NO2
CAS No.	94-09-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31 mg/mL (187.7 mM)

Ethanol: 31 mg/mL (187.7 mM)

References and Literature

1. Wang GK, et al. Pflugers Arch, 1998, 435(2), 293-302. 2. Pinto LM, et al. Biophys Chem, 2000, 87(2-3), 213-223. 3. Quan C, et al. Biophys J, 1996, 70(1), 194-201. 4. Caballero R, et al. Cardiovasc Res, 2002, 56(1), 104-117. 5. Nathan D, et al. Pharm Res, 1990, 7(11), 1147-1151.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Ion Channel Inhibitor Library Clinical Compound Library Drug-Fragment Library ReFRAME Related Library Bioactive Compound Library Pediatric Drug Library

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Keywords

Benzocaine 94-09-7 Immunology/Inflammation Membrane transporter/Ion channel Others Sodium Channel MRP Na channels 34584 Na+ channels Inhibitor inhibit inhibitor

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