1. Anti-infection
  2. Beta-lactamase Bacterial Antibiotic
  3. Cloxacillin sodium

Cloxacillin sodium is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin sodium can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.

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Cloxacillin sodium Chemical Structure

Cloxacillin sodium Chemical Structure

CAS No. : 642-78-4

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Based on 3 publication(s) in Google Scholar

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Description

Cloxacillin sodium is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin sodium can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins[1][2][3].

IC50 & Target

Tetracycline

 

In Vitro

Cloxacillin sodium (0-2048 µg/mL; 20-24 h) shows good antibacterial activity for S. aureus 8325-4 and DU1090 with MIC values both of 0.125 µg/mL[1].
Cloxacillin sodium (0.015625 μg/mL; 6 h) inhibits the hemolytic activity of Hlα in vitro, and this inhibition is not only more pronounced when combined with TZ and TZ, but also suppresses the inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins[1].

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

Cell Viability Assay[1]

Cell Line: S. aureus 8325-4, S. aureus DU1090 (an Hlα-deleted strain)
Concentration: 0-2048 µg/mL
Incubation Time: 20-24 h
Result: Inhibited S. aureus 8325-4 and DU1090 with MIC values both of 0.125 µg/mL.

Western Blot Analysis[1]

Cell Line: S. aureus 8325-4
Concentration: 0.015625 μg/mL (combines with Thioridazine (TZ, 0.25 μg/mL) and Tetracycline (TC, 0.03125 μg/mL)).
Incubation Time: 6 h
Result: Inhibited the expression of Hlα and the inhibition was more pronounced when combined with TZ and TC.

Western Blot Analysis[1]

Cell Line: RAW264.7 cells (exposes to S. aureus 8325-4/DU1090 or pure Hlα)
Concentration: 0.015625 μg/mL (combines with TZ (0.25 μg/mL) and TC (0.03125 μg/mL)).
Incubation Time: 6 h
Result: Inhibited the activation of MAPKs, NF-кB and NLRP3-related proteins thereby inhibiting the inflammatory response when combined with TC and TZ.
In Vivo

Cloxacillin sodium (1.6125 mg/kg; s.c.; 12-h intervals for 72 h) protects mice from S. aureus peritonitis in vivo when combines with Thioridazine and Tetracycline[1].
Cloxacillin sodium (7.5 mg/per; i.p.; twice daily from day 3 for 3 days) develops less severe synovitis and reduces bone erosions when combines with anti-IL-15 antibodies[3].

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

Animal Model: Female BALB/c mice (6-week-old; peritonitis model)[1].
Dosage: 1.6125 mg/kg (combines with TC (3.125 mg/kg) and TZ (25 mg/kg))
Administration: Subcutaneous injection; 12-h intervals for 72 h.
Result: Reduced the degree of inflammatory cell infiltration in the mouse lung tissue and alveolar structures tended to be normal.
Significantly reduced the pathological changes in spleen and liver tissue, as well as decreased the CFU counts of S. aureus in the peritoneal cavity.
Animal Model: Female wildtype C57BL/6 mice (8-week-old; systemic S. aureus-induced arthritis model)
Dosage: 7.5 mg/per (combines with 25 µg/per anti-IL-15 antibodies)
Administration: Intraperitoneal injection; twice daily from day 3 (after bacterial inoculation) and stopped at day 6.
Result: Showed activities of reducing severe synovitis and bone erosions when combined with anti-IL-15 antibodies.
Clinical Trial
Molecular Weight

457.86

Formula

C19H17ClN3NaO5S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(C(C(C=CC=C1)=C1Cl)=NO2)=C2C)N[C@H]3[C@](SC(C)4C)([H])N(C3=O)[C@H]4C(O[Na])=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (218.41 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 2.1841 mL 10.9204 mL 21.8407 mL
5 mM 0.4368 mL 2.1841 mL 4.3681 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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 (5.46 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 (5.46 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.
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).

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

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

Purity: 98.03%

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). 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
DMSO 1 mM 2.1841 mL 10.9204 mL 21.8407 mL 54.6018 mL
5 mM 0.4368 mL 2.1841 mL 4.3681 mL 10.9204 mL
10 mM 0.2184 mL 1.0920 mL 2.1841 mL 5.4602 mL
15 mM 0.1456 mL 0.7280 mL 1.4560 mL 3.6401 mL
20 mM 0.1092 mL 0.5460 mL 1.0920 mL 2.7301 mL
25 mM 0.0874 mL 0.4368 mL 0.8736 mL 2.1841 mL
30 mM 0.0728 mL 0.3640 mL 0.7280 mL 1.8201 mL
40 mM 0.0546 mL 0.2730 mL 0.5460 mL 1.3650 mL
50 mM 0.0437 mL 0.2184 mL 0.4368 mL 1.0920 mL
60 mM 0.0364 mL 0.1820 mL 0.3640 mL 0.9100 mL
80 mM 0.0273 mL 0.1365 mL 0.2730 mL 0.6825 mL
100 mM 0.0218 mL 0.1092 mL 0.2184 mL 0.5460 mL
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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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