2. Membrane Transporter/Ion Channel Immunology/Inflammation NF-κB
  3. NF-κB Sodium Channel NOD-like Receptor (NLR)
  4. Articaine hydrochloride

Articaine hydrochloride  (Synonyms: Hoe-045)

Cat. No.: HY-B0516 Purity: 99.38%
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Handling Instructions Technical Support

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).

For research use only. We do not sell to patients.

Articaine hydrochloride Chemical Structure

Articaine hydrochloride Chemical Structure

CAS No. : 23964-57-0

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Articaine hydrochloride:

Articaine hydrochloride Related Antibodies

Top Publications Citing Use of Products

View All NF-κB Isoform Specific Products:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8 Nav1.9

View All NOD-like Receptor (NLR) Isoform Specific Products:

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NLRP3 NLRP1 NOD1 NOD2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1][2][3].

IC50 & Target

NLRP3

 

In Vivo

Articaine (20 mg/kg, 40 mg/kg; intraperitoneal injection; single dose) hydrochloride 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 hydrochloride (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.

Animal Model: Swiss albino mice with LPS-induced acute kidney injury model[2]
Dosage: 20 mg/kg, 40 mg/kg Articaine
Administration: Intraperitoneal injection; single dose
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.
Clinical Trial
Molecular Weight

320.84

Formula

C13H21ClN2O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(C)NCCC)NC(C(C)=CS1)=C1C(OC)=O.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (311.68 mM; Need ultrasonic)

DMSO : 100 mg/mL (311.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1168 mL 15.5841 mL 31.1682 mL
5 mM 0.6234 mL 3.1168 mL 6.2336 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (311.68 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.1168 mL 15.5841 mL 31.1682 mL 77.9205 mL
5 mM 0.6234 mL 3.1168 mL 6.2336 mL 15.5841 mL
10 mM 0.3117 mL 1.5584 mL 3.1168 mL 7.7920 mL
15 mM 0.2078 mL 1.0389 mL 2.0779 mL 5.1947 mL
20 mM 0.1558 mL 0.7792 mL 1.5584 mL 3.8960 mL
25 mM 0.1247 mL 0.6234 mL 1.2467 mL 3.1168 mL
30 mM 0.1039 mL 0.5195 mL 1.0389 mL 2.5973 mL
40 mM 0.0779 mL 0.3896 mL 0.7792 mL 1.9480 mL
50 mM 0.0623 mL 0.3117 mL 0.6234 mL 1.5584 mL
60 mM 0.0519 mL 0.2597 mL 0.5195 mL 1.2987 mL
80 mM 0.0390 mL 0.1948 mL 0.3896 mL 0.9740 mL
100 mM 0.0312 mL 0.1558 mL 0.3117 mL 0.7792 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Articaine hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Articaine23964-57-0Hoe-045Hoe045Hoe 045NF-κBSodium ChannelNOD-like Receptor (NLR)Nuclear factor-κBNuclear factor-kappaBNa channelsNa+ channelsdentalamidepain reliefkidney injuryLPSInhibitorinhibitorinhibit

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