2. Anti-infection
  3. Beta-lactamase Bacterial
  4. Eravacycline dihydrochloride

Eravacycline dihydrochloride  (Synonyms: TP-434 dihydrochloride; TP-434-046)

Cat. No.: HY-16980A Purity: 98.98%
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Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent.

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

Eravacycline dihydrochloride Chemical Structure

Eravacycline dihydrochloride Chemical Structure

CAS No. : 1334714-66-7

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5 mg USD 450 In-stock
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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of Eravacycline dihydrochloride:

Eravacycline dihydrochloride Related Antibodies

Top Publications Citing Use of Products

    Eravacycline dihydrochloride 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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    Metallo-β-lactamase

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent.

    In Vitro

    Eravacycline is potent antibiotic against A. baumannii, including isolates that are resistant to sulbactam, SM 7338, and BAY 41-6551. Eravacycline shows greater activity than BAY 41-6551, and colistin. The Eravacycline dihydrochloride 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.

    Eravacycline dihydrochloride Related Antibodies
    In Vivo

    Eravacycline dihydrochloride 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. 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

    631.48

    Formula

    C27H33Cl2FN4O8
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    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.[H]Cl.[H]Cl
    Shipping

    Shipping with dry ice.
    Storage

    -80°C, protect from light, stored under nitrogen

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (158.36 mM; Need ultrasonic)

    DMSO : ≥ 50 mg/mL (79.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5836 mL 7.9179 mL 15.8358 mL
    5 mM 0.3167 mL 1.5836 mL 3.1672 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    * 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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    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: ≥ 5.5 mg/mL (8.71 mM); Clear solution

      This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 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: ≥ 5.5 mg/mL (8.71 mM); Clear solution

      This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 50 mg/mL (79.18 mM); Clear solution; Need ultrasonic

    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: 98.98%

    COA (251 KB) HNMR (323 KB) RP-HPLC (247 KB) LCMS (263 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [3][5]

    Rats: 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[3].

    Mice: 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[5].

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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 1.5836 mL 7.9179 mL 15.8358 mL 39.5895 mL
    5 mM 0.3167 mL 1.5836 mL 3.1672 mL 7.9179 mL
    10 mM 0.1584 mL 0.7918 mL 1.5836 mL 3.9590 mL
    15 mM 0.1056 mL 0.5279 mL 1.0557 mL 2.6393 mL
    20 mM 0.0792 mL 0.3959 mL 0.7918 mL 1.9795 mL
    25 mM 0.0633 mL 0.3167 mL 0.6334 mL 1.5836 mL
    30 mM 0.0528 mL 0.2639 mL 0.5279 mL 1.3197 mL
    40 mM 0.0396 mL 0.1979 mL 0.3959 mL 0.9897 mL
    50 mM 0.0317 mL 0.1584 mL 0.3167 mL 0.7918 mL
    60 mM 0.0264 mL 0.1320 mL 0.2639 mL 0.6598 mL
    H2O 80 mM 0.0198 mL 0.0990 mL 0.1979 mL 0.4949 mL
    100 mM 0.0158 mL 0.0792 mL 0.1584 mL 0.3959 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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    Eravacycline dihydrochloride 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:

    Eravacycline1334714-66-7TP-434 TP-434-046TP434TP 434Beta-lactamaseBacterialβ-lactamaseInhibitorinhibitorinhibit

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