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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 23964-58-1
- 分子式: C13H20N2O3S
- 分子量:284.37
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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NLRP3 |
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.
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Animal Model:Swiss albino mice with LPS-induced acute kidney injury model[2]
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Dosage:20 mg/kg, 40 mg/kg
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Administration:Intraperitoneal injection; single dose
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Result:Reduced serum BUN, creatinine, and cystatin C levels, alleviated renal histopathological damage, inhibited production of TNF-α, IL-6, IL-1β, and reduced MDA levels while increasing SOD and GSH activities.
Suppressed NF-κB activation, TLR4 expression, and NLRP3 inflammasome pathway, and restored Bcl-2/Bax ratio.
化学情報
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CAS 番号 23964-58-1
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分子量 284.37
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分子式 C13H20N2O3S
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SMILES
O=C(C(C)NCCC)NC(C(C)=CS1)=C1C(OC)=O
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別名
Hoe-045 free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Articaine 関連分類
HY-B0516A 関連分類
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