Articaine

• Description :

  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 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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• Isoform :

  NLRP3

• CAS Number :

  [23964-58-1]