1. Anti-infection
  2. Bacterial Antibiotic
  3. Mupirocin

Mupirocin  (Synonyms: BRL-4910A; Pseudomonic acid)

Cat. No.: HY-B0958 Purity: 98.04%
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Mupirocin (BRL-4910A, Pseudomonic acid) is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.

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Mupirocin Chemical Structure

Mupirocin Chemical Structure

CAS No. : 12650-69-0

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Based on 1 publication(s) in Google Scholar

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Description

Mupirocin (BRL-4910A, Pseudomonic acid) is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis[1][2].

In Vitro

Mupirocin (BRL-4910A, Pseudomonic acid) (0-100 μM; 48 h) shows antibacterial effect against staphylococci, streptococci and certain gram-negative bacteria, with MIC values range from 0.06-0.25 μg/mL (MIC50 =0.12 μg/mL, MIC90 =0.25 μg/mL)[1].
Mupirocin is highly bound (95% bound) to human serum protein, thus results in activity inhibition in the presence of human serum[1].
Mupirocin apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis[2].
Mupirocin (2% ointment) reduces pro-inflammatory cytokines IL-1β and IL-17 level, decreases tumor necrosis factor-alpha (TNF-α) expression, and increases the leavel of vascular endothelial growth factor (VEGF)[4].
Mupirocin inhibits MS (S. epidermidis ATCC 12228), MR (S. epidermidis (Se56-99)), and VIR (S. epidermidis (Se43-98)) with MICs of 0.25, 1.26, 1.59 mg/L[5].
Note: MIC, the minimum inhibition concentration.

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

Cell Viability Assay[1]

Cell Line: Staphylococcus aureus
Concentration: 0-100 μM/mL
Incubation Time: 24, 48 hours
Result: Resulted in a 90 to 99% reduction at 24 h, with MIC values ranged from 0.12-1.0 μM/mL and MBC values ranged from 4.0-32 μM/mL at 48 h.
In Vivo

MRSA: Meticillin-resistant Staphylococcus aureus
Mupirocin (BRL-4910A, Pseudomonic acid) is well absorbed after oral and parenteral administration but serum antibiotic concentrations were short-lived as a result of extensive degradation to the antibacterially inactive metabolite, monic acid A[1].
Mupirocin (2% ointment; external administration; twice daily; 3-6 d) decreases the total bacterial loads in the skin lesions with either topical treatment[3].
Mupirocin (2% ointment; external administration; 4 d) alleviates MRSA-infected pressure ulcers in mice[4].
Mupirocin (100 mg/mL; s.c.; 7 d) exerts prevention efficacy against vascular prosthetic graft infection due to Staphylococcus epidermidis[5].

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

Animal Model: MRSA skin infection model in mice (10-12 weeks old)[3]
Dosage: 2% ointment
Administration: External administration; twice daily; 3-6 days
Result: Reduced the total bacterial loads in the skin lesions, and decreased by 2.0, 5.1 log10 CFU on day 3 and 6, respectively.
Animal Model: Diabetic pressure ulcer mouse model (33.2-39.2 g)[4]
Dosage: 2% ointment
Administration: External administration; 4 days
Result: Resulted less superficial mats of bacterial colonies, and improved histopathology evaluation.
Animal Model: Adult male Wistar rats (weight 275-325 g)[5]
Dosage: Impregnated with 100 μg of mupirocin/mL; segments:1.5 cm *1 cm2
Administration: Subcutaneous implantation; 7 days
Result: Resulted in preventing S. epidermidis infection of the graft in a rat model with spontaneously bound to collagen-sealed Dacron grafts.
Clinical Trial
Molecular Weight

500.62

Formula

C26H44O9

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@H]1[C@@](CO[C@@H](C/C(C)=C/C(OCCCCCCCCC(O)=O)=O)[C@@H]1O)([H])C[C@H]2[C@@]([C@@H](C)[C@@H](O)C)([H])O2

Structure Classification
Initial Source

Pseudomonas fluorescens

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 : ≥ 100 mg/mL (199.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9975 mL 9.9876 mL 19.9752 mL
5 mM 0.3995 mL 1.9975 mL 3.9950 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.

  • 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 (4.99 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 (4.99 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).
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

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
DMSO 1 mM 1.9975 mL 9.9876 mL 19.9752 mL 49.9381 mL
5 mM 0.3995 mL 1.9975 mL 3.9950 mL 9.9876 mL
10 mM 0.1998 mL 0.9988 mL 1.9975 mL 4.9938 mL
15 mM 0.1332 mL 0.6658 mL 1.3317 mL 3.3292 mL
20 mM 0.0999 mL 0.4994 mL 0.9988 mL 2.4969 mL
25 mM 0.0799 mL 0.3995 mL 0.7990 mL 1.9975 mL
30 mM 0.0666 mL 0.3329 mL 0.6658 mL 1.6646 mL
40 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2485 mL
50 mM 0.0400 mL 0.1998 mL 0.3995 mL 0.9988 mL
60 mM 0.0333 mL 0.1665 mL 0.3329 mL 0.8323 mL
80 mM 0.0250 mL 0.1248 mL 0.2497 mL 0.6242 mL
100 mM 0.0200 mL 0.0999 mL 0.1998 mL 0.4994 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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