1. Anti-infection
  2. Bacterial
  3. Eravacycline

Eravacycline (Synonyms: TP-434)

Cat. No.: HY-16980
Handling Instructions

Eravacycline is a potent and broad-spectrum antibacterial agent.

For research use only. We do not sell to patients.

Eravacycline Chemical Structure

Eravacycline Chemical Structure

CAS No. : 1207283-85-9

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Description

Eravacycline is a potent and broad-spectrum antibacterial agent.

IC50 & Target

Antibacterial[1]

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].

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].

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[[email protected]@]3([H])C[[email protected]@]4([H])[[email protected]](N(C)C)C(O)=C(C(N)=O)C([[email protected]@]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.

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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Keywords:

EravacyclineTP-434TP434TP 434BacterialInhibitorinhibitorinhibit

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