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Mecillinam (Synonyms: Amdinocillin, FL 1060, Penicillin Hx)

Catalog No.GC45932 Copy One-Click Copy Product Info

Mecillinam is a penicillin derivative that is selective and highly effective against Gram-negative bacteria.

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Mecillinam Chemical Structure

Cas No.: 32887-01-7

Size Price Stock Qty
10 mg
$30.00
In stock
50 mg
$60.00
In stock
100 mg
$98.00
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Sample solution is provided at 25 µL, 10mM.



Description of Mecillinam

Mecillinam is a penicillin derivative that is selective and highly effective against Gram-negative bacteria [1]. Mecillinam specifically targets the class B penicillin-binding protein (PBP) 2 in Escherichia coli and causes the loss of rod shape and the formation of large spherical cells that eventually lyse [2]. Mecillinam has been widely used to alleviate urinary tract infections and kill various drug-resistant bacteria[3].

In vitro, Mecillinam treatment (1000µg/ml) for 30 minutes significantly reduced the respiratory burst activity of polymorphonuclear neutrophil leukocytes (PMN) [4].

In vivo, Mecillinam treatment via subcutaneous injection of a 1mg dose of Mecillinam, three times a day, for a duration of 3 days, significantly reduced the load of Escherichia coli in the urine, kidneys, and bladder of the mice in the urinary tract infection model[5].

References:
[1] Jansåker F, Frimodt-Møller N, Benfield T L, et al. Mecillinam for the treatment of acute pyelonephritis and bacteremia caused by Enterobacteriaceae: a literature review[J]. Infection and drug resistance, 2018: 761-771.
[2] Lai G C, Cho H, Bernhardt T G. The mecillinam resistome reveals a role for peptidoglycan endopeptidases in stimulating cell wall synthesis in Escherichia coli[J]. PLoS genetics, 2017, 13(7): e1006934.
[3] Hawser S, Morrissey I, Kothari N, et al. Activity of mecillinam against USA urinary tract clinical isolates from 2017 to 2020 including isolates resistant to comparator antibiotics[J]. Journal of Global Antimicrobial Resistance, 2024, 39: 137-143.
[4] Dosogne, Hoeben, Burvenich, et al. Effect of cephapirin and mecillinam on the phagocytic and respiratory burst activity of neutrophil leukocytes isolated from bovine blood[J]. Journal of veterinary pharmacology and therapeutics, 1998, 21(6): 421-427.
[5] Zykov I N, Frimodt-Møller N, Småbrekke L, et al. Efficacy of mecillinam against clinical multidrug-resistant Escherichia coli in a murine urinary tract infection model[J]. International journal of antimicrobial agents, 2020, 55(2): 105851.

Protocol of Mecillinam

Animal experiment [1]:

Animal models

Female outbred albino OF1 mice

Preparation Method

Female outbred albino OF1 mice were kept under alternating 12-h light and dark cycles, an ambient temperature of 23±2°C, and a relative humidity of 55±5% with ad libitum access to water. Three days prior to inoculation, drinking water was substituted with 5% glucose solution. Anaesthetized mice were inoculated in the bladder with 50µl of Escherichia coli suspension containing 109CFU/ml using a sterilized plastic catheter, which was further retracted. Urine was collected on Day 1 (after 24h) to verify infection, and then treatment was subsequently initiated. Mice were given 1mg Mecillinam/mouse or vehicle (0.9% NaCl solution) as 0.2ml subcutaneous injections. On Day 4, urine was collected from mice by gently pressing on the abdomen. The mice were then euthanized by cervical dislocation. The remaining urine was added to tubes, and the bladder and both kidneys were aseptically removed for analysis.

Dosage form

1mg; three times a day for 3 days; s.c.

Applications

Mecillinam treatment significantly reduced the load of Escherichia coli in the urine, kidneys, and bladder of the mice in the urinary tract infection model.

References:
[1] Zykov I N, Frimodt-Møller N, Småbrekke L, et al. Efficacy of mecillinam against clinical multidrug-resistant Escherichia coli in a murine urinary tract infection model[J]. International journal of antimicrobial agents, 2020, 55(2): 105851.

Chemical Properties of Mecillinam

Cas No. 32887-01-7 SDF
Synonyms Amdinocillin, FL 1060, Penicillin Hx
Canonical SMILES O=C(O)[C@@H](C(C)(C)S1)N2[C@@]1([H])[C@H](N=CN3CCCCCC3)C2=O
Formula C15H23N3O3S M.Wt 325.4
Solubility Chloroform: 30 mg/ml Storage 4°C, protect from light, stored under nitrogen
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Mecillinam

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.0731 mL 15.3657 mL 30.7314 mL
5 mM 614.6 μL 3.0731 mL 6.1463 mL
10 mM 307.3 μL 1.5366 mL 3.0731 mL
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In vivo Formulation Calculator (Clear solution) of Mecillinam

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

Quality Control & SDS

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Reviews

Review for Mecillinam

Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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