2. Anti-infection Neuronal Signaling Membrane Transporter/Ion Channel
  3. Bacterial Antibiotic GABA Receptor
  4. Cefepime

Cefepime (BMY-28142) is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC50 of 21.115 mM and a Ki of 35.092 mM. Cefepime inhibits hPON1 via a non-competitive mechanism and blocks GABAA receptors. Cefepime penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.

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CAS No. : 88040-23-7

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Customer Review

Based on 18 publication(s) in Google Scholar

Other Forms of Cefepime:

Cefepime Related Antibodies

Top Publications Citing Use of Products

    Cefepime purchased from MedChemExpress. Usage Cited in: J Antimicrob Chemother. 2026 Feb 2;81(3):dkag034.  [Abstract]

    Activities of new β-lactam/β-lactamase inhibitors (Cefepime, et al.) against AmpC-hyperproducing E. cloacae complex and Klebsiella aerogenes were evaluated.

    Cefepime purchased from MedChemExpress. Usage Cited in: Infect Genet Evol. 2025 Sep:133:105780.  [Abstract]

    Antibiotic sensitivity of K. pneumoniae Kp81 and its derivatives.

    Cefepime purchased from MedChemExpress. Usage Cited in: Vet Microbiol. 2024 May:292:110046.

    MICs for 16 antimicrobial agents against 381 strains of P. multocida from pigs.
    a AMP: ampicillin, AMX: amoxicillin, CEF: ceftiofur, CIP: ciprofloxacin, COL: colistin, CPM: Cefepime, DOX: doxycycline, ENR: enrofloxacin, ERY: erythromycin, FFC: florfenicol, GEN: gentamicin, IPM: imipenem, SPT: spectinomycin, TET: tetracycline, TGC: tigecycline, TIL: tilmicosin.
    b NA: breakpoint not available.
    c veterinary-specific breakpoints applicable to porcine P. multocida from CLSI VET01S ED7:2024; light grey shading – susceptible, dark grey shading – intermediate, black shading – resistant.

    Cefepime purchased from MedChemExpress. Usage Cited in: J Antibiot (Tokyo). 2023 Apr;76(4):225-235.  [Abstract]

    Susceptibility patterns of E. coli isolates (n = 140) towards different β-Lactams singly and in combination with β-Lactamase inhibitors (CFP Cefoperazone, CAZ Ceftazidime, FEP Cefepime). The results showed that cephalosporins were effective against E. coli isolates at the following rates: cefoperazone (52.9%), ceftazidime (43.5%), and Cefepime (32.1%).

    View All Antibiotic Isoform Specific Products:

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    Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Cefepime (BMY-28142) is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC50 of 21.115 mM and a Ki of 35.092 mM. Cefepime inhibits hPON1 via a non-competitive mechanism and blocks GABAA receptors. Cefepime penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase[1][2][3][4].

    IC50 & Target

    β-lactam

     

    Cellular Effect
    Cell Line Type Value Description References
    HeLa IC50
    1700 μM
    Compound: Cefepime
    TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.02 uM) in OCTN2-expressing HeLa cells
    TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.02 uM) in OCTN2-expressing HeLa cells
    		[PMID: 10636865]
    In Vitro

    Cefepime (18 h) potently inhibits most isolates of Gram-negative aerobic bacteria. Among these pathogens, the MIC90 value is ≤1 mg/L for most Enterobacteriaceae, 16 mg/L for Pseudomonas aeruginosa, and ≤0.12 mg/L for Haemophilus influenzae, Neisseria gonorrhoeae and Branhamella catarrhalis[4].
    Cefepime (18-48 h) inhibits Gram-positive bacterial isolates, with an MIC90 value of ≤ 4 mg/L against staphylococci and an MIC90 value of ≤ 0.25 mg/L against most streptococci, but shows limited activity against Enterococcus faecalis, Listeria monocytogenes and Bacteroides species[4].
    Cefepime exhibits stable in vitro activity across different culture media, pH values, and inoculum sizes. For most isolates, the difference between its MIC and MBC values is extremely small, but the MBC values of Pseudomonas aeruginosa and Staphylococcus aureus in human serum are higher[4].
    Cefepime (2-8×MIC; 2-24 h) exhibits concentration-dependent bactericidal activity against Enterobacter cloacae (with the strongest activity and no regrowth observed at 8×MIC), sustained bactericidal activity against Pseudomonas aeruginosa, but only limited transient activity against Methicillin (HY-121544)-resistant Staphylococcus aureus[4].
    Cefepime (1 mM) exhibits high stability against almost all tested plasmid-mediated and chromosome-mediated bacterial β-lactamases, and is only slightly hydrolyzed by the PSE-2 enzyme[4].
    Cefepime is a weak inhibitor of most bacterial β-lactamases, exhibiting only weak activity against Proteus vulgaris Ic enzyme and Pseudomonas aeruginosa Id enzyme, with an IC50 value of > 400 mg/L against the key clinical β-lactamases TEM-1 and P99[4].
    Cefepime exhibited only marginal differences in MIC values among Escherichia colipermeability mutants, whereas an 8-fold difference was observed among Pseudomonas aeruginosapermeability mutants, indicating that its ability to enhance bacterial cell wall penetration is limited[4].

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

    Cefepime Related Antibodies
    In Vivo

    Cefepime induces bacterial stasis in a neutropenic murine thigh infection model infected with Enterobacteriaceae and Klebsiella pneumoniae, under the condition that the unbound drug concentration remains above the MIC for 0-37.7% of the dosing interval[2].
    Cefepime (250-500 mg/kg; intravenous bolus) does not increase the susceptibility to pentylenetetrazol (PTZ)-induced convulsions in normal male ICR mice[3].
    Cefepime (250-500 mg/kg; intravenous bolus) significantly increases the average seizure grade to 3.3 in the low-current electroshock-induced seizure model of normal male ICR mice, while the 250 mg/kg dose increases the average seizure grade to 2.0[3].
    Cefepime (500 mg/kg; intravenous bolus) induces convulsions in 2 out of 3 normal male ICR mice, and elicits electroencephalogram spike waves in the parietal cortex of 1 mouse following low-current electroshock stimulation[3].
    Cefepime (500 mg/kg; intravenous bolus) significantly increases the average seizure grade induced by low-current electroconvulsive shock to 4.0 in cornea-kindled male ICR mice[3].

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

    Animal Model: Male CD-1 mice[4]
    Dosage: 80 mg/kg
    Administration: I.p.
    Result: Significantly prolonged the half-life of cefepime and all mice survived at 18-22 mg/kg cisplatin, and when pretreatment with 26 mg/kg cisplatin significantly decreased survival with the half-life of cefepime was not significantly longer than of 18 mg/kg cisplatin.
    Molecular Weight

    480.56

    Formula

    C19H24N6O5S2
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    C[N+]1(CC(CS[C@]2([H])[C@@H]3NC(/C(C4=CSC(N)=N4)=N\OC)=O)=C(C([O-])=O)N2C3=O)CCCC1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 116.67 mg/mL (242.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 100 mg/mL (208.09 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0809 mL 10.4045 mL 20.8091 mL
    5 mM 0.4162 mL 2.0809 mL 4.1618 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    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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    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: ≥ 2.08 mg/mL (4.33 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.33 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.86%

    SDS (394 KB)

    COA (255 KB) HNMR (261 KB) RP-HPLC (205 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.0809 mL 10.4045 mL 20.8091 mL 52.0226 mL
    5 mM 0.4162 mL 2.0809 mL 4.1618 mL 10.4045 mL
    10 mM 0.2081 mL 1.0405 mL 2.0809 mL 5.2023 mL
    15 mM 0.1387 mL 0.6936 mL 1.3873 mL 3.4682 mL
    20 mM 0.1040 mL 0.5202 mL 1.0405 mL 2.6011 mL
    25 mM 0.0832 mL 0.4162 mL 0.8324 mL 2.0809 mL
    30 mM 0.0694 mL 0.3468 mL 0.6936 mL 1.7341 mL
    40 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3006 mL
    50 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0405 mL
    60 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8670 mL
    80 mM 0.0260 mL 0.1301 mL 0.2601 mL 0.6503 mL
    100 mM 0.0208 mL 0.1040 mL 0.2081 mL 0.5202 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Cefepime Related Classifications

    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.

    Keywords:

    Cefepime88040-23-7BMY-28142BMY28142BMY 28142BacterialAntibioticGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorcross the blood-brain barriercephalosporinantibacterialneurotoxicityInhibitorinhibitorinhibit

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