1. NF-κB Anti-infection
  2. NF-κB Bacterial
  3. Erdosteine

Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects.

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

Erdosteine Chemical Structure

Erdosteine Chemical Structure

CAS No. : 84611-23-4

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation[1][2]. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects[3].

IC50 & Target[1]

NF-κB

 

In Vitro

Erdosteine is an oral mucolytic agent used as an expectorant in various chronic respiratory diseases. Erdosteine exerts anti-inflammatory effects by inhibiting NF-κB activation in LPS-stimulated mouse macrophages. However, Erdosteine does not inhibit LPS induced phosphorylation of the Akt and MAPK pathways. To evaluate the toxic effects of Erdosteine on macrophages, cell viability is analyzed. Treatment with 1, 10, or 100 μg/mL Erdosteine does not produce detectable cytotoxicity. Treatment with LPS (1 μg/mL) induced IκBα degradation in RAW 264.7 cells, and maximal degradation is observed after 10 min. RAW 264.7 cells are pretreated with the indicated concentrations of Erdosteine for 6 h and then stimulated with LPS (1 μg/mL) for 10 min. Pretreatment with Erdosteine does not have any effect on the baseline amount of IκBα. Treatment with DMSO alone at a volume equal to that used for Erdosteine delivery does not have any effect on the baseline amount of IκBα. The amount of IκBα is decreased by treatment with LPS for 10 min, and pretreatment with Erdosteine at the indicated concentration and time effectively inhibits IκBα degradation[1].

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

In Vivo

Twenty-six male mice are divided into four groups as follows: group 1, control; group 2, Erdosteine-treated; group 3, Methotrexate (MTX)-treated; and group 4, Methotrexate+Erdosteine treated. On the first day of experiment, a single dose of Methotrexate is intraperitoneally administered to groups 3 and 4, although a daily single dose of Erdosteine is orally administered to group 2 and 4 for 7 days. At the end of the experiment, the testes of the animals are removed and weighed. The levels of total antioxidant capacity and total oxidative stress, and myeloperoxidase activity in the Methotrexate group are higher than the control group (p<0.05). Lipid peroxidation levels are not changed in Methotrexate group compared with control group. In conclusion, Erdosteine can effectively protect the testes in Methotrexate-induced toxicity. Erdosteine administration with Methotrexate improves testicular injures, as indicated by appearance of spermatogenesis in seminiferous tubules[2].

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

Clinical Trial
Molecular Weight

249.31

Formula

C8H11NO4S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CSCC(NC(CCS1)C1=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (200.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 6.67 mg/mL (26.75 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0111 mL 20.0554 mL 40.1107 mL
5 mM 0.8022 mL 4.0111 mL 8.0221 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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)

Mass
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Concentration
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Volume
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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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Volume (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: ≥ 3.25 mg/mL (13.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 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: ≥ 3.25 mg/mL (13.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 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: 6.67 mg/mL (26.75 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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Cell Assay
[1]

The murine macrophage/monocyte cell line RAW264.7 are maintained as monolayers in Dulbecco’s modified Eagle’s medium (DMEM) containing 10 % fetal bovine serum, 60 U/mL Penicillin, and 100 μg/mL Streptomycin at 37.8°C in 5 % CO2. The cell viability is quantified using a colorimetric tetrazolium compound MTS assay. Briefly, 1×104 cells incubated with various concentrations of Erdosteine (1, 10, or 100 μg/mL) for 24 h are treated with 10 μL of MTS solution (5 mg/mL) for 45 min. The cells are then lysed with isopropyl alcohol, and the absorbance is read at the wavelength of 540 nm[1].

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

Animal Administration
[2]

Mice[2]
Twenty-six male C57BL/6 mice (8 weeks, 20-30 g) are randomly divided into four groups. In control group (n=6); mice are treated the 0.5 mL of saline as a placebo intraperitoneally (i.p.). In Erdosteine group (n=6), mice are treated with Erdosteine orally (gavage; 10 mg/kg) for 7 days. In this study, low-dose MTX are used because high-dose (20-40 mg/kg) MTX has anti-inflammatory and immunosuppressive activity. Mice in MTX group (n=7) are injected with single dose of i.p. MTX (10 mg/kg). In MTX+Erdosteine group (n=7), mice are injected with single dose of i.p. MTX (10 mg/kg) the first day and Erdosteine is given orally (10 mg/kg) to the animals starting the first day for 7 days. After the last administration of the drug, all rats fasted about 12 hours, but have free access to water. And then, the animals are sacrificed by cervical dislocation at the end of the experiment. Following sacrifice, the testes are quickly removed from the mice. Right testes specimens are fixed in 10% neutral-buffered formaldehyde solution for histological assessment[2].

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.0111 mL 20.0554 mL 40.1107 mL 100.2768 mL
5 mM 0.8022 mL 4.0111 mL 8.0221 mL 20.0554 mL
10 mM 0.4011 mL 2.0055 mL 4.0111 mL 10.0277 mL
15 mM 0.2674 mL 1.3370 mL 2.6740 mL 6.6851 mL
20 mM 0.2006 mL 1.0028 mL 2.0055 mL 5.0138 mL
25 mM 0.1604 mL 0.8022 mL 1.6044 mL 4.0111 mL
DMSO 30 mM 0.1337 mL 0.6685 mL 1.3370 mL 3.3426 mL
40 mM 0.1003 mL 0.5014 mL 1.0028 mL 2.5069 mL
50 mM 0.0802 mL 0.4011 mL 0.8022 mL 2.0055 mL
60 mM 0.0669 mL 0.3343 mL 0.6685 mL 1.6713 mL
80 mM 0.0501 mL 0.2507 mL 0.5014 mL 1.2535 mL
100 mM 0.0401 mL 0.2006 mL 0.4011 mL 1.0028 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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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.

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