1. Anti-infection
  2. Bacterial
  3. Eravacycline dihydrochloride

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

Cat. No.: HY-16980A Purity: 97.21%
Handling Instructions

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 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
25 mg USD 180 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Eravacycline dihydrochloride:

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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 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. 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

631.48

Formula

C₂₇H₃₃Cl₂FN₄O₈

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.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (237.54 mM; Need ultrasonic)

H2O : 50 mg/mL (79.18 mM; Need ultrasonic)

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
10 mM 0.1584 mL 0.7918 mL 1.5836 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

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

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 7.5 mg/mL (11.88 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 7.5 mg/mL (11.88 mM); Clear solution

*All of the co-solvents are provided by MCE.
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
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Keywords:

EravacyclineTP-434 TP-434-046TP434TP 434BacterialInhibitorinhibitorinhibit

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Product Name:
Eravacycline dihydrochloride
Cat. No.:
HY-16980A
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