1. Anti-infection
  2. Beta-lactamase Bacterial Antibiotic
  3. Eravacycline

Eravacycline is a potent and broad-spectrum antibacterial agent.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Eravacycline dihydrochloride) usually boasts enhanced water solubility and stability.

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Eravacycline Chemical Structure

Eravacycline Chemical Structure

CAS No. : 1207283-85-9

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Top Publications Citing Use of Products

    Eravacycline purchased from MedChemExpress. Usage Cited in: Microbiol Spectr. 2022 Dec 8;e0323822.  [Abstract]

    The MIC distributions of Eravacycline against 43 M. fortuitum isolates. The y axis shows the number of strains with each MIC value, with the specific numbers shown above the bars.
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    Description

    Eravacycline is a potent and broad-spectrum antibacterial agent.

    IC50 & Target

    Tetracycline

     

    In Vitro

    Eravacycline is potent antibiotic against A. baumannii, including isolates that are resistant to sulbactam, imipenem/meropenem, levofloxacin, and amikacin/tobramycin. Eravacycline shows greater activity than the comparators of the tetracycline class, levofloxacin, amikacin, tobramycin, and colistin. The eravacycline MIC50/90 values are 0.5/1 mg/L[1]. Eravacycline shows inhibitory effects on six E. coli with MICs ranging from 0.125 to 0.25 mg/L[2]. Eravacycline dihydrochloride is a synthetic antibiotic, with inhibits bacterial protein synthesis through binding to the 30S ribosomal subunit. Eravacycline displays broad spectrum activity against gram-negative bacteria in the panel except P. aeruginosa, as well as excellent activity against major gram-positive pathogens, including methicillin-resistant S. aureus. Eravacycline also displays potent ribosomal inhibition[3]. Eravacycline shows potent broad-spectrum activity against 90% of the isolates (MIC90) in each panel at concentrations ranging from ≤0.008 to 2 μg/mL for all species panels except those of Pseudomonas aeruginosa and Burkholderia cenocepacia (MIC90 values of 32 μg/mL for both organisms). Eravacycline is active against multidrug-resistant bacteria, including those expressing extended-spectrum β-lactamases and mechanisms conferring resistance to other classes of antibiotics, including carbapenem resistance[4].

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

    In Vivo

    Mice are treated with two-fold increasing doses (range 3.125 to 50 mg/kg) of eravacycline every 12 hours. The mean fAUC/MIC magnitude associated with net stasis and 1-log kill endpoint are 27.97±8.29 and 32.60±10.85, respectively[2]. Eravacycline is active in multiple murine models of infection against clinically important Gram-positive and Gram-negative pathogens. Eravacycline is efficacious in mouse septicemia models, demonstrating 50% protective dose values of ≤1 mg/kg of body weight once a day (q.d.) against Staphylococcus aureus, including tetracycline-resistant isolates of methicillin-resistant S. aureus (MRSA), and Streptococcus pyogenes. The PD50 values against Escherichia coli isolates are 1.2 to 4.4 mg/kg q.d[5].

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

    Clinical Trial
    Molecular Weight

    558.56

    Formula

    C27H31FN4O8

    CAS No.
    SMILES

    O=C(NC(C(O)=C1C2=O)=CC(F)=C1C[C@@]3([H])C[C@@]4([H])[C@H](N(C)C)C(O)=C(C(N)=O)C([C@@]4(O)C(O)=C32)=O)CN5CCCC5

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Purity & Documentation
    References
    Animal Administration
    [3][5]

    Rats[3]
    Pharmacokinetic (PK) parameters are determined in Sprague−Dawley rats. Animals are fasted overnight (minimum of 12 h) and given a single oral (10 mg/kg) or IV dose (1 mg/kg) of eravacycline followed by a sampling scheme for 24 h. Plasma and dosing solution concentrations are determined by TurboIonspray LC/MSMS analysis using appropriate standard curves. PK parameters are calculated by noncompartmental analysis.
    Mice[5]
    Eravacycline is formulated in sterile 0.9% saline. BALB/c mice are inoculated with 0.2 mL of prepared bacterial inoculum via intravenous injection to seed the kidney. Animals are administered antibiotics (eravacycline) at 10 mL/kg i.v. via the tail vein 12 and 24 h postinfection. Then the bacterial burden is determined.

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

    References
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    Eravacycline Related Classifications

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    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.

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