| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Meropenem sodium targets penicillin-binding proteins (PBPs), which are bacterial cell wall-synthesizing enzymes. By binding to multiple PBPs with high affinity, it inhibits the final transpeptidation step of peptidoglycan synthesis, disrupting bacterial cell wall integrity and leading to cell lysis and death. The compound is highly stable against inactivation by the majority of β-lactamases and kidney dehydropeptidase I.
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|---|---|
| ln Vitro |
Meropenem sodium exhibits an extended spectrum of antibacterial activity with low minimum inhibitory concentrations (MICs) against a wide range of clinical isolates. Against Enterobacteriaceae, the MIC90 ranges from 0.03 mg/L to 0.125 mg/L. Meropenem shows excellent activity against extended-spectrum β-lactamase (ESBL)-producing Klebsiella pneumoniae, most Acinetobacter species, Pseudomonas aeruginosa, and anaerobic species including Clostridium difficile (MIC90 = 1.0 mg/L), Clostridium perfringens, and other Clostridium species. It demonstrates activity against susceptible and resistant Neisseria gonorrhoeae (MIC range 0.02-0.06 mg/mL), Haemophilus influenzae (MIC range 0.03-0.12 mg/mL), and Haemophilus ducreyi (MIC range 0.015-0.12 mg/mL). Against ESBL-producing E. coli and K. pneumoniae isolates, meropenem displays a median MIC of 0.125 μg/mL (range 0.03-32 μg/mL), with greater in vitro potency compared to ertapenem. Meropenem is far more stable in agar than imipenem; the mean MIC of control strains remained constant at 0.05 mg/L over 10 days, whereas imipenem's mean MIC rose to 0.24 mg/L after two days and 3.4 mg/L after ten days.
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| ln Vivo |
In a neutropenic mouse thigh infection model, human-simulated meropenem dosing (1 g every 8 h) produced free-drug time above MIC (fT>MIC) values ranging from 93% for susceptible isolates (MIC 0.03 μg/mL) to 30% for resistant isolates (MIC 8 μg/mL). Meropenem displayed sustained efficacy against ESBL-producing E. coli and K. pneumoniae isolates with elevated ertapenem MICs (≥2 μg/mL), achieving bacterial reductions ranging from a static effect to a 1-log reduction (fT>MIC = 30-65%). In a murine model of advanced carbapenem-resistant Acinetobacter baumannii (CRAB) pneumonia, intratracheal meropenem (20 mg/kg every 8 h) resulted in a 100% survival rate, which was significantly superior to imipenem (50%), colistimethate sodium (33%), and saline control (0%) (p < 0.001 vs. control and CMS groups; p = 0.006 vs. imipenem group). Meropenem also demonstrated superior tissue penetration, bacterial clearance, normalization of wet lung-to-body weight ratio, and down-regulation of pro-inflammatory cytokine levels in the lungs.
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| Enzyme Assay |
Traditional enzyme or receptor binding assay protocols (such as surface plasmon resonance, isothermal titration calorimetry, or radioligand binding) for meropenem sodium are not described in the available literature. The primary methods for characterizing meropenem's activity are microbiological susceptibility tests. Minimum inhibitory concentration (MIC) determination by agar dilution: The agar dilution method is used to determine MICs following Clinical and Laboratory Standards Institute (CLSI) recommendations. Test bacteria are cultured, and serial dilutions of meropenem are incorporated into agar plates. Bacterial suspensions are spotted onto the plates, incubated, and the lowest concentration inhibiting visible growth is recorded as the MIC. Agar stability testing: The stability of meropenem in agar is determined indirectly by plotting the geometric mean MIC of control strains over a period of two weeks. The mean MIC is monitored at intervals (e.g., day 0, day 2, day 10) to assess drug stability in the test medium.
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| Animal Protocol |
Neutropenic mouse thigh infection model: Female ICR mice weighing approximately 25 g are rendered transiently neutropenic by intraperitoneal injections of cyclophosphamide at doses of 150 mg/kg and 100 mg/kg at 4 days and 1 day before bacterial inoculation, respectively. Three days prior to inoculation, mice receive a single intraperitoneal injection of 5 mg/kg uranyl nitrate to induce a predictable degree of renal impairment. Thigh infections are established by intramuscular injection of bacterial inoculum (approximately 10⁵ CFU). Human-simulated meropenem dosing regimens are designed to approximate the free-drug percent time above the MIC observed in humans following meropenem at 1 g every 8 hours.
Murine acute pneumonia model (CRAB): Six- to eight-week-old inbred BALB/c female mice (20-22 g) are anesthetized with sodium pentobarbital (70 mg/kg). Acute pneumonia is established by intratracheal inoculation of 50 μL bacterial suspension containing 2.5 × 10⁷ CFU of A. baumannii plus 10% porcine mucin. Four hours post-inoculation (when acute pneumonia is established), treatment is initiated. Meropenem is administered intratracheally at 20 mg/kg every 8 hours in a 25 μL volume. Control groups receive 0.85% saline, imipenem/cilastatin (30/30 mg/kg every 8 h), or colistimethate sodium (166,666 U/kg every 8 h). Survival rates are recorded every 12 hours until 72 hours post-inoculation. For bacterial clearance assessment, surviving mice are sacrificed at 24, 48, and 72 hours, and homogenized lung samples are cultured to quantify bacterial load (log10 CFU/mg). Cytokine levels (TNF-α, IL-1β, IL-6, MIP-2) in bronchoalveolar lavage fluid are measured by ELISA. |
| ADME/Pharmacokinetics |
Meropenem sodium is a hydrophilic, small molecule with a low volume of distribution (approximately 0.3 L/kg) and very low protein binding (<2%). The drug is primarily eliminated by the kidneys, as only the unbound fraction is available for glomerular filtration (major elimination pathway). Approximately 70% of a dose is excreted unchanged in urine, with the remaining dose undergoing nonrenal clearance primarily through conversion to an open-ring metabolite. The elimination half-life is approximately 1 hour in healthy adults but is prolonged in patients with renal impairment. Creatinine clearance has the greatest impact on meropenem clearance. Dose adjustments are required for patients with creatinine clearance ≤ 50 mL/min. The volume of distribution is described by the equation V = 33.00 × (weight/73)²·⁰⁷, while total body clearance is described by CL = 3.68 + 0.22 × (residual diuresis/100). In critically ill patients with septic shock and continuous renal replacement therapy (CRRT), residual diuresis significantly influences meropenem total clearance. The drug exhibits linear pharmacokinetics. For optimal bactericidal activity, the pharmacokinetic/pharmacodynamic target is maintaining unbound drug concentrations above the minimum inhibitory concentration (fT>MIC) for 40% of the dosing interval, though some data suggest higher targets (100% fT>MIC or 100% fT>4×MIC) may be beneficial in critically ill patients.
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| Toxicity/Toxicokinetics |
Meropenem sodium is contraindicated in patients with known hypersensitivity to product components or with a history of anaphylactic reactions to beta-lactams. Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients receiving beta-lactams. Contraindicated where the administration of sodium or chloride could be clinically detrimental.
Warnings and precautions: Severe cutaneous adverse reactions (including Stevens-Johnson syndrome) have been reported; discontinue immediately if experienced. Seizures and other adverse central nervous system experiences have been reported during treatment. Co-administration with valproic acid or divalproex sodium reduces serum concentration of valproic acid, potentially increasing the risk of breakthrough seizures. Clostridioides difficile-associated diarrhea (ranging from mild diarrhea to fatal colitis) has been reported. In patients with renal dysfunction, thrombocytopenia has been observed. Most common adverse reactions (incidence ≥ 2%): headache, nausea, constipation, diarrhea, anemia, vomiting, and rash. Experiments have shown meropenem to have a low toxicity profile and, in contrast to similar compounds, no central nervous system toxicity. Solutions containing sodium ions should be used with great care, if at all, in patients where the administration of sodium could be detrimental. |
| References | |
| Additional Infomation |
Meropenem sodium (CAS: 211238-34-5) has the IUPAC name sodium (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-carboxylate. The compound has a logP of -1.376, polar surface area of 138.31 Ų, and 6 rotatable bonds. It is soluble in water and stable under recommended storage conditions. For research use only, not for human use; we do not sell to patients. Meropenem is available as a sterile powder for injection, typically formulated with sodium carbonate to enhance solubility and stability. The drug is on the World Health Organization's List of Essential Medicines.
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| Molecular Formula |
C17H24N3NAO5S
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|---|---|
| Molecular Weight |
405.44
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| Exact Mass |
405.133
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| CAS # |
211238-34-5
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| Related CAS # |
211238-34-5 (sodium); Meropenem;96036-03-2;Meropenem-d6;1217976-95-8; 96036-03-2 (free); 119478-56-7 (hydrate);
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| PubChem CID |
23718739
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| Appearance |
Typically exists as solids at room temperature
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| LogP |
0
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
685
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC1C2C(C(=O)N2C(=C1SC3CC(NC3)C(=O)N(C)C)C(=O)[O-])C(C)O.[Na+]
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| InChi Key |
UBQRNADYCUXRBD-NACOAMSHSA-M
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| InChi Code |
InChI=1S/C17H25N3O5S.Na/c1-7-12-11(8(2)21)16(23)20(12)13(17(24)25)14(7)26-9-5-10(18-6-9)15(22)19(3)4;/h7-12,18,21H,5-6H2,1-4H3,(H,24,25);/q;+1/p-1/t7-,8-,9+,10+,11-,12-;/m1./s1
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| Chemical Name |
sodium (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-carboxylate
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| Synonyms |
Meropenem sodium salt; DTXSID50635806; 1-Azabicyclo(3.2.0)hept-2-ene-2-carboxylic acid, 3-(((3S,5S)-5-((dimethylamino)carbonyl)-3-pyrrolidinyl)thio)-6-((1R)-1-hydroxyethyl)-4-methyl-7-oxo-, monosodium salt, (4R,5S,6S)-; 1-Azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid, 3-[[(3S,5S)-5-[(dimethylamino)carbonyl]-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-, monosodium salt, (4R,5S,6S)-; RefChem:1054866;
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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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4665 mL | 12.3323 mL | 24.6646 mL | |
| 5 mM | 0.4933 mL | 2.4665 mL | 4.9329 mL | |
| 10 mM | 0.2466 mL | 1.2332 mL | 2.4665 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.
Products are for research use only; We do not sell to patients
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