| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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Purity: ≥98%
| ln Vitro |
Strong antibiotic eryavacycline is effective against isolates of A. baumannii, including those resistant to sulbactam, BAY 41-6551, and SM 7338. Eravacycline is more active than colistin and BAY 41-6551. The MIC50/90 values of eravacycline dihydrochloride are 0.5/1 mg/L [1]. Six E. coli strains with MICs ranging from 0.125 to 0.25 mg/L exhibit inhibitory effects when exposed to eravacycline[2]. Eravacycline dihydrochloride is a synthetic antibiotic that binds to the 30S ribosomal subunit to prevent bacteria from synthesizing proteins. Eravacycline exhibits good activity against significant gram-positive pathogens, such as methicillin-resistant S. aureus, and broad spectrum activity against gram-negative bacteria in the panel, with the exception of P. aeruginosa. Additionally, eravacycline exhibits strong ribosomal inhibition[3].In all species panels, eravacycline exhibits strong broad-spectrum activity against 90% of the isolates (MIC90) at concentrations ranging from ≤0.008 to 2 μg/mL, with the exception of Pseudomonas aeruginosa and Burkholderia cenocepacia, which both have MIC90 values of 32 μg/mL. Eravacycline exhibits efficacy against bacteria that are resistant to multiple drugs, such as those that express extended-spectrum β-lactamases and mechanisms that confer resistance to other antibiotic classes, such as carbapenem resistance[4].
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| ln Vivo |
Several murine infection models demonstrate the efficacy of eravacycline dihydrochloride against Gram-positive and Gram-negative pathogens that are clinically significant. Eravacycline shows 50% protective dose values of ≤1 mg/kg of body weight once a day (q.d.) against Staphylococcus aureus in mouse septicemia models, indicating its effectiveness. In relation to Escherichia coli isolates, the PD50 values range from 1.2 to 4.4 mg/kg q.d[5].
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| Animal Protocol |
Rats: Sprague-Dawley rats are used to determine pharmacokinetic (PK) parameters. After fasting for at least 12 hours, the animals receive a single oral dose of eravacycline (10 mg/kg) or an IV dose (1 mg/kg), and then they participate in a 24-hour sampling scheme. Using the relevant standard curves, TurboIonspray LC/MSMS analysis determines the concentrations of the dosing solution and plasma. Noncompartmental analysis is used to calculate PK parameters[3].
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| References |
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| Molecular Formula |
C27H33CL2FN4O8
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|---|---|
| Molecular Weight |
631.48
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| Exact Mass |
558.21
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| Elemental Analysis |
C, 51.36; H, 5.27; Cl, 11.23; F, 3.01; N, 8.87; O, 20.27
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| CAS # |
1334714-66-7
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| Related CAS # |
Eravacycline;1207283-85-9
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| Appearance |
Solid powder
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| SMILES |
O=C(C1=C(O)[C@@H](N(C)C)[C@@](C[C@@]2([H])C(C(C3=C(O)C(NC(CN4CCCC4)=O)=CC(F)=C3C2)=O)=C5O)([H])[C@@]5(O)C1=O)N.[H]Cl.[H]Cl
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| InChi Key |
JYCNMRVZELJVAW-RZVFYPHASA-N
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| InChi Code |
InChI=1S/C27H31FN4O8.2ClH/c1-31(2)20-13-8-11-7-12-14(28)9-15(30-16(33)10-32-5-3-4-6-32)21(34)18(12)22(35)17(11)24(37)27(13,40)25(38)19(23(20)36)26(29)39;;/h9,11,13,20,34,36-37,40H,3-8,10H2,1-2H3,(H2,29,39)(H,30,33);2*1H/t11-,13-,20-,27-;;/m0../s1
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| Chemical Name |
(4S,4aS,5aR,12aS)-4-(Dimethylamino)-7-fluoro-3,10,12,12a-tetrahydroxy-1,11-dioxo-9-((pyrrolidin-1-ylacetyl)amino)-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide dihydrochloride
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| Synonyms |
TP-434-046; TP 434-046; TP434-046; TP-434; TP 434; TP434; Eravacycline HCl; Eravacycline hydrochloride.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (3). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~158.36 mM)
DMSO : ≥ 50 mg/mL (~79.18 mM） |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.5 mg/mL (8.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 55.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5.5 mg/mL (8.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 55.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5.5 mg/mL (8.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 5.5 mg/mL (8.71 mM) Solubility in Formulation 5: 50 mg/mL (79.18 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Single-dose plasma pharmacokinetics of eravacycline.
In vivodose fractionation with eravacycline using a neutropenic murine thigh infection model.Antimicrob Agents Chemother.2017 Jun 27;61(7). pii: e00250-17. |
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 Impact of pharmacodynamic regression of thein vivodose fractionation study with eravacycline against E. coli ATCC 25922.Antimicrob Agents Chemother.2017 Jun 27;61(7). pii: e00250-17. |
 In vivodose-effect of eravacycline against six E. coli (EC) strains using a neutropenic murine thigh infection model.
In vivodose-effect of eravacycline against six E. coli isolates using a neutropenic murine thigh infection model.Antimicrob Agents Chemother.2017 Jun 27;61(7). pii: e00250-17. |
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