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Meropenem

In stock
Catalog No.
A5124
β-lactam antibiotic of the carbapenem subclass
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$80.00
In stock
25mg
$50.00
In stock
50mg
$60.00
In stock
100mg
$90.00
In stock
250mg
$180.00
In stock

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Meropenem is an ultra-broad-spectrum injectable β-lactam antibiotic used to treat a wide variety of infections. Meropenem has been shown to inhibit penicillinase-negative, -positive and methicillin-susceptible staphylococci [1].

In vitro: The meropenem MICs for penicillin-resistant Streptococcus pneumoniae were higher than for the penicillin-susceptible strains but the organisms remained susceptible. Clinical susceptibility in vitro to meropenem was defined by MICs of ≤ 4 mg/L, intermediate susceptibility by MICs of 8 mg/L and MICs of ≥ 16 mg/L define resistance; equivalent figures for zones of growth inhibition were ≥ 14 (susceptible), 12-13 (intermediate) and ≤ 11 (resistant) mm[1].Meropenem was 2- to 4-fold more active than imipenem against Gram-negative organisms and its spectrum of antimicrobial activity was wider than those of all other drugs tested.Meropenem inhibited all anaerobic bacteria at less than or equal to 8 mg/l and 0.25 mg/l inhibited 50% of strains. Meropenem MICs were not significantly influenced by high inocula and the drug was generally bactericidal [2].Meropenem bound most strongly to penicillin-binding protein 2 of Escherichia coli and Pseudomonas aeruginosa, and to penicillin-binding proteins 1 of Staphylococcus aureus [3].Meropenem had one identified metabolite, a β-lactam ring-opened form which is devoid of microbiological activity[4].

In vivo: In rabbits, meropenem significantly increased the plamsa total clearance of valproate to about 1.5 times compared to the control (6.09 mL/min/kg vs. 4.28 mL/min/kg). Meropenem significantly increased the urinary excretion of valproate- glucuronide in rabbits [5].

References:
[1].  Edwards J R. Meropenem: a microbiological overview[J]. Journal of Antimicrobial Chemotherapy, 1995, 36(suppl A): 1-17.
[2].  Jones R N, Barry A L, Tbornsberry C. In-vitro studies of meropenem[J]. Journal of Antimicrobial Chemotherapy, 1989, 24(suppl A): 9-29.
[3].  Yang Y, Bhachech N, Bush K. Biochemical comparison of imipenem, meropenem and biapenem: permeability, binding to penicillin-binding proteins, and stability to hydrolysis by β-lactamases[J]. Journal of Antimicrobial Chemotherapy, 1995, 35(1): 75-84.
[4].  Drusano G L, Hutchison M. The pharmacokinetics of meropenem[J]. Scandinavian journal of infectious diseases.Supplementum, 1994, 96: 11-16.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt383.46
Cas No.96036-03-2
FormulaC17H25N3O5S
Solubility≥19.15mg/mL in DMSO, <2.34 mg/mL in EtOH, ≥9.88 mg/mL in H2O with ultrasonic
Chemical Name(4R,5S,6S)-3-[(3S,5S)-5-(dimethylcarbamoyl)pyrrolidin-3-yl]sulfanyl-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
SDFDownload SDF
Canonical SMILESCC1C2C(C(=O)N2C(=C1SC3CC(NC3)C(=O)N(C)C)C(=O)O)C(C)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

1116 strains including 659 Gram-negative bacteria, 271 Gram-positive organisms, 96 strains of more rarely isolated species and 90 strictly anaerobic bacteria.

Preparation method

The solubility of this compound in DMSO is >19.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0-25 mg/l

Applications

In 659 Gram-negative bacteria, Meropenem exhibited the widest spectrum of activity against these listed species and inhibited all but nine strains (MICs≥16mg/l). In 271 Gram-positive organisms tested, only two methicillin-resistant staphylococci and five Enterococcus faecium strains had meropenem MICs of ≥16mg/l. In 90 strains of strictly anaerobic organisms, Meropenem was quite active against these bacteria with an overall MIC90 of 1 mg/1.

Animal experiment [2]:

Animal models

Septic rat model of Klebsiella pneumoniae

Dosage form

30 mg/kg and an equivalent dose of the drug-loaded nanoparticle dispersion; single intraperitoneal injection

Application

In septic rat model of Klebsiella pneumoniae, treatment with free meropenem exhibited 30% mortality, which was not statistically significant, as compared to the control untreated rats (50% mortality). However, all rats treated with the drug-loaded nanoparticle dispersions survived during the 48 h, suggesting a significant improvement of survival rate. Infected animals treated with free meropenem showed no significant reduction of blood bacterial count, while the drug-loaded nanoparticles significantly reduced blood bacterial counts.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Jones R N, Barry A L, Tbornsberry C. In-vitro studies of meropenem[J]. Journal of Antimicrobial Chemotherapy, 1989, 24(suppl A): 9-29.

[2]. Abdelkader A1, El-Mokhtar MA2, Abdelkader O1, et al. Ultrahigh antibacterial efficacy of meropenem-loaded chitosan nanoparticles in a septic animal model. Carbohydr Polym. 2017 Oct 15;174:1041-1050.

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