Articaine  (Synonyms: Hoe-045 free base)

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].

Articaine (20 mg/kg, 40 mg/kg; intraperitoneal injection; single dose) can significantly reduce serum urea nitrogen, creatinine and cystatin C levels, alleviate renal tissue pathological damage, inhibit the release of inflammatory factors such as TNF-α, IL-6, and IL-1β, and exert anti-inflammatory effects by inhibiting NF-κB activation and NLRP3 inflammasome pathway in the lipopolysaccharide (LPS)-induced acute kidney injury model of Swiss albino mice^[2].
Articaine (0.5 mM, 1 mM; immersion for 1 h) can enhance the anesthetic effect in the zebrafish model, inhibiting the tactile response rate by 100% and reducing the heart rate by 60%. In combination with nanolipid carriers (NLCs), it can prolong the duration of anesthesia^[3].

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

284.37

C₁₃H₂₀N₂O₃S

23964-58-1

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]