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

Cloxacillin sodium monohydrate is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin sodium monohydrate 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 monohydrate Chemical Structure

Cloxacillin sodium monohydrate Chemical Structure

CAS No. : 7081-44-9

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Based on 3 publication(s) in Google Scholar

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Description

Cloxacillin sodium monohydrate is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin sodium monohydrate 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 monohydrate (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 monohydrate (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 monohydrate (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 monohydrate (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

475.88

Formula

C19H19ClN3NaO6S

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)(C)[C@@H]4C(O[Na])=O)([H])N4C3=O.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (210.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (105.07 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1014 mL 10.5069 mL 21.0137 mL
5 mM 0.4203 mL 2.1014 mL 4.2027 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 (protect from light, stored under nitrogen). 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

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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 (5.25 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 (5.25 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 (210.14 mM); Clear solution; Need ultrasonic

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

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(per animal)

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Dosing volume
(per animal)

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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 (protect from light, stored under nitrogen). 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 2.1014 mL 10.5069 mL 21.0137 mL 52.5343 mL
5 mM 0.4203 mL 2.1014 mL 4.2027 mL 10.5069 mL
10 mM 0.2101 mL 1.0507 mL 2.1014 mL 5.2534 mL
15 mM 0.1401 mL 0.7005 mL 1.4009 mL 3.5023 mL
20 mM 0.1051 mL 0.5253 mL 1.0507 mL 2.6267 mL
25 mM 0.0841 mL 0.4203 mL 0.8405 mL 2.1014 mL
30 mM 0.0700 mL 0.3502 mL 0.7005 mL 1.7511 mL
40 mM 0.0525 mL 0.2627 mL 0.5253 mL 1.3134 mL
50 mM 0.0420 mL 0.2101 mL 0.4203 mL 1.0507 mL
60 mM 0.0350 mL 0.1751 mL 0.3502 mL 0.8756 mL
80 mM 0.0263 mL 0.1313 mL 0.2627 mL 0.6567 mL
100 mM 0.0210 mL 0.1051 mL 0.2101 mL 0.5253 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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