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；腹腔注射；单次) 在瑞士白化小鼠的脂多糖 (LPS) 诱导急性肾损伤模型中，能显著降低血清尿素氮、肌酐和胱抑素 C 水平，减轻肾脏组织病理损伤，抑制 TNF-α、IL-6、IL-1β 等炎症因子释放，并通过抑制 NF-κB 激活及 NLRP3 炎症小体通路发挥抗炎作用^[2]。
Articaine (0.5 mM、1 mM；浸泡 1 h) 在斑马鱼模型中，可增强麻醉效果，使触反应抑制率达 100%，心率降低 60%，且与纳米脂质载体 (NLC) 联用可延长麻醉持续时间^[3]。

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

284.37

C₁₃H₂₀N₂O₃S

23964-58-1

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]