Articaine

Articaine (Hoe-045) is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC50 of 15.8 μM for open-state Na+ channels, and IC50 of 40.6 μM and 378 μM for inactivated and resting-state Na+ channels, respectively. Articaine exerts local anesthetic activity by inhibiting Na+ influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury) [1][2][3].

Product Specifications

CAS Number

[23964-58-1]

Product Name Alternative

Hoe-045 (free base)

UNSPSC

12352005

Hazard Statement

H302

Target

NF-κB; NOD-like Receptor (NLR) ; Sodium Channel

Type

Reference compound

Related Pathways

Immunology/Inflammation; Membrane Transporter/Ion Channel; NF-κB

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/articaine.html

Solubility

10 mM in DMSO

Smiles

O=C(C(C)NCCC)NC(C(C)=CS1)=C1C(OC)=O

Molecular Formula

C13H20N2O3S

Molecular Weight

284.37

Precautions

P264-P270-P330-P501

References & Citations

[1]Wang GK, et al. State-dependent block of Na+ channels by articaine via the local anesthetic receptor. J Membr Biol. 2009 May;229 (1) :1-9.|[2]Zhao G, et al. Local anesthetic articaine ameliorates LPS-induced acute kidney injury via inhibition of NF-ĸB activation and the NLRP3 inflammasome pathway. J Biochem Mol Toxicol. 2020 Oct;34 (10) :e22554.|[3]Rodrigues da Silva GH, et al. Articaine in functional NLC show improved anesthesia and anti-inflammatory activity in zebrafish. Sci Rep. 2020 Nov 12;10 (1) :19733.