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Mupirocin (BRL-4910A; Pseudomonic acid) is an potent isoleucyl t-RNA synthetase inhibitor and an orally bioactive antibiotic isolated from Pseudomonas fluorescens. It is used in the treatment of bacterial skin infections. Mupirocin is an antibiotic of the monoxycarbolic acid class. The effect of Mupirocin is concentration dependent, being bacteriostatic at low concentrations and bactericidal at high concentrations. It is used topically and is effective against Gram-positive bacteria, including MRSA. Mupirocin is a mixture of several pseudomonic acids, with pseudomonic acid A (PA-A) constituting greater than 90% of the mixture.
| ln Vitro |
With MIC values ranging from 0.06-0.25 μg/mL (MIC50 = 0.12 μg/mL, MIC90 = 0.25 μg/mL), mupirocin (BRL-4910A, pseudomonoic acid) calcium hydrate (0-100 μM; 48 h) exhibits antibacterial activity against staphylococci, streptococci, and some gram-negative bacteria[1].
The presence of human serum inhibits the activity of mugirocin calcium hydrate due to its strong 95% binding to human serum protein[1].
It appears that the antimicrobial activity of mugirocin calcium hydrate is achieved by reversibly inhibiting isoleucyl-transfer RNA, which in turn inhibits the synthesis of bacterial proteins and RNA[2]. Mupirocin calcium hydrate (2% ointment) decreases the expression of tumor necrosis factor-alpha (TNF-α), increases the leavel of vascular endothelial growth factor (VEGF), and decreases the levels of pro-inflammatory cytokines IL-1β and IL-17[4]. With MICs of 0.25, 1.26, and 1.59 mg/L, mugirocin calcium hydrate inhibits MS (S. epidermidis ATCC 12228), MR (S. epidermidis (Se56-99)), and VIR (S. epidermidis (Se43-98))[5]. |
|---|---|
| ln Vivo |
MRSA: Staphylococcus aureus resistant to meticillin
Following oral and parenteral administration, mupirocin (BRL-4910A, pseudomononic acid) calcium is well absorbed; however, the prolonged breakdown of the antibiotic to the antibacterially inactive metabolite monic acid A resulted in short-lived serum antibiotic concentrations [1]. Using either topical treatment, mugirocin calcium (2% ointment; external administration; twice daily; 3-6 d) reduces the overall bacterial loads in the skin lesions[3]. Mice with pressure ulcers infected with MRSA are treated with 2% ointment of mupirocin calcium administered externally every 4 days[4]. Staphylococcus epidermidis-caused vascular prosthetic graft infection can be prevented with mugirocin calcium (100 mg/mL; s.c.; 7 d)[5]. |
| Cell Assay |
Cell Line: Staphylococcus aureus
Concentration: 0-100 μM/mL Incubation Time: 24, 48 hours Result: produced a 90–99% reduction at 24 hours, with MIC and MBC values ranging from 0.12-1.0 μM/mL and 4.0–32 μM/mL, respectively, at 48 hours. |
| Animal Protocol |
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: decreased the overall amount of bacteria present in the skin lesions, with reductions of 2.0 and 5.1 log10 CFU on days three and six, respectively. |
| References |
|
| Molecular Formula |
C52H90CAO20
|
|---|---|
| Molecular Weight |
1077.35288
|
| Exact Mass |
1,074.57
|
| Elemental Analysis |
C, 58.08; H, 8.44; Ca, 3.73; O, 29.76
|
| CAS # |
115074-43-6
|
| Related CAS # |
Mupirocin;12650-69-0;Mupirocin calcium;104486-81-9
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| Appearance |
Solid powder
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| SMILES |
O.O.[Ca+2].C[C@H](O)[C@H](C)[C@@H]1O[C@H]1C[C@H]2CO[C@@H](C\C(=C\C(=O)OCCCCCCCCC(=O)[O-])\C)[C@H](O)[C@@H]2O.C[C@H](O)[C@H](C)[C@@H]3O[C@H]3C[C@H]4CO[C@@H](C\C(=C\C(=O)OCCCCCCCCC(=O)[O-])\C)[C@H](O)[C@@H]4O
|
| InChi Key |
DDHVILIIHBIMQU-YJGQQKNPSA-L
|
| InChi Code |
InChI=1S/2C26H44O9.Ca.2H2O/c2*1-16(13-23(30)33-11-9-7-5-4-6-8-10-22(28)29)12-20-25(32)24(31)19(15-34-20)14-21-26(35-21)17(2)18(3)27/h2*13,17-21,24-27,31-32H,4-12,14-15H2,1-3H3,(H,28,29)2*1H2/q+2/p-2/b2*16-13+/t2*17-,18-,19-,20-,21-,24+,25-,26-/m00.../s1
|
| Chemical Name |
calcium 9-(((E)-4-((2S,3R,4R,5S)-3,4-dihydroxy-5-(((2S,3S)-3-((2S,3S)-3-hydroxybutan-2-yl)oxiran-2-yl)methyl)tetrahydro-2H-pyran-2-yl)-3-methylbut-2-enoyl)oxy)nonanoate dihydrate
|
| Synonyms |
Mupirocin calcium salt; Calcium Mupirocin Dihydrate; Mupirocin Calcium Hydrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~185.64 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (2.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9282 mL | 4.6410 mL | 9.2820 mL | |
| 5 mM | 0.1856 mL | 0.9282 mL | 1.8564 mL | |
| 10 mM | 0.0928 mL | 0.4641 mL | 0.9282 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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