Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent.
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Eravacycline dihydrochloride Chemical Structure
CAS No. : 1334714-66-7
This product is a controlled substance and not for sale in your territory.
Based on 24 publication(s) in Google Scholar
Other Forms of Eravacycline dihydrochloride:
Eravacycline
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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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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.
*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
ConcentrationSolventMass
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
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.
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 μLDMSO 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 μLDMSO 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.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5.5 mg/mL (8.71 mM); Clear solution
This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (55.0 mg/mL) to 900 μLCorn oil, and mix evenly.
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).
[1]. Seifert H, et al. In-vitro activity of the novel fluorocycline eravacycline against carbapenem non-susceptible Acinetobacter baumannii. Int J Antimicrob Agents. 2017 Jul 10.
[Content Brief]
[2]. Zhao M, et al. In Vivo Pharmacodynamic Target Assessment of Eravacycline against Escherichia coli in a Murine Thigh Infection Model. Antimicrob Agents Chemother. 2017 Jun 27;61(7).
[Content Brief]
[3]. Xiao XY, et al. Fluorocyclines: a potent, broad spectrum antibacterial agent. J Med Chem. 2012 Jan 26;55(2):597-605.
[Content Brief]
[4]. Sutcliffe JA, et al. Antibacterial activity of eravacycline (TP-434), a novel fluorocycline, against hospital and community pathogens. Antimicrob Agents Chemother. 2013 Nov;57(11):5548-58.
[Content Brief]
[5]. Grossman TH, et al. Eravacycline (TP-434) is efficacious in animal models of infection. Antimicrob Agents Chemother. 2015 May;59(5):2567-71.
[Content Brief]
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
[1]. Seifert H, et al. In-vitro activity of the novel fluorocycline eravacycline against carbapenem non-susceptible Acinetobacter baumannii. Int J Antimicrob Agents. 2017 Jul 10.
[Content Brief]
[2]. Zhao M, et al. In Vivo Pharmacodynamic Target Assessment of Eravacycline against Escherichia coli in a Murine Thigh Infection Model. Antimicrob Agents Chemother. 2017 Jun 27;61(7).
[Content Brief]
[3]. Xiao XY, et al. Fluorocyclines: a potent, broad spectrum antibacterial agent. J Med Chem. 2012 Jan 26;55(2):597-605.
[Content Brief]
[4]. Sutcliffe JA, et al. Antibacterial activity of eravacycline (TP-434), a novel fluorocycline, against hospital and community pathogens. Antimicrob Agents Chemother. 2013 Nov;57(11):5548-58.
[Content Brief]
[5]. Grossman TH, et al. Eravacycline (TP-434) is efficacious in animal models of infection. Antimicrob Agents Chemother. 2015 May;59(5):2567-71.
[Content Brief]
[1]. Seifert H, et al. In-vitro activity of the novel fluorocycline eravacycline against carbapenem non-susceptible Acinetobacter baumannii. Int J Antimicrob Agents. 2017 Jul 10.
[2]. Zhao M, et al. In Vivo Pharmacodynamic Target Assessment of Eravacycline against Escherichia coli in a Murine Thigh Infection Model. Antimicrob Agents Chemother. 2017 Jun 27;61(7).
[3]. Xiao XY, et al. Fluorocyclines: a potent, broad spectrum antibacterial agent. J Med Chem. 2012 Jan 26;55(2):597-605.
[4]. Sutcliffe JA, et al. Antibacterial activity of eravacycline (TP-434), a novel fluorocycline, against hospital and community pathogens. Antimicrob Agents Chemother. 2013 Nov;57(11):5548-58.
[5]. Grossman TH, et al. Eravacycline (TP-434) is efficacious in animal models of infection. Antimicrob Agents Chemother. 2015 May;59(5):2567-71.
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
ConcentrationSolventMass
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.
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.
