23964-58-1
Chemical Structure
Articaine
Synonym(s): Hoe-045 free base
- CAS No.: 23964-58-1
- Formula:C13H20N2O3S
- Molecular Weight:284.37
IUPAC Name: methyl 4-methyl-3-(2-(propylamino)propanamido)thiophene-2-carboxylate
InChIKey: QTGIAADRBBLJGA-UHFFFAOYSA-N
SMILES: O=C(C(C)NCCC)NC(C(C)=CS1)=C1C(OC)=O
Biological Activity: 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].
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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). | |||||||||||||||||||||
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Articaine (Standard) | ≥98% | Articaine (Standard) is the analytical standard of Articaine (HY-B0516A). This product is intended for research and analytical applications. Articaine (Hoe-045) hydrochloride 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 hydrochloride 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 hydrochloride can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury). | ||||||||||||||||||||
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- [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]
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