Eravacycline (dihydrochloride)
Eravacycline (dihydrochloride) Basic information
- Product Name:
- Eravacycline (dihydrochloride)
- Synonyms:
-
- Eravacycline (dihydrochloride)
- Eravacyline
- TP-434-046
- ERAVACYCLINE 2HCL
- TP-434 2HCl
- Eravacycline HCl
- Eravacycline diHClide (TP-434 diHClide)
- (4S,4aS,5aR,12aS)-4-(Dimethylamino)-7-fluoro-3,10,12,12a-tetrahydroxy-1,11-dioxo-9-(2-(pyrrolidin-1-yl)acetamido)-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide dihydrochloride
- CAS:
- 1334714-66-7
- MF:
- C27H32ClFN4O8
- MW:
- 595.02
- Mol File:
- 1334714-66-7.mol
Eravacycline (dihydrochloride) Chemical Properties
- storage temp.
- -80°C, protect from light, stored under nitrogen,unstable in solution, ready to use.
- form
- Solid
- color
- Light yellow to yellow
- Water Solubility
- Water : 50 mg/mL (79.18 mM)
- InChIKey
- XCNSMXGRPDKXPD-WWKMUIPSNA-N
- SMILES
- O[C@@]12C(C(C(=O)N)=C(O)[C@@H](N(C)C)[C@]1([H])C[C@]1([H])CC3=C(C=C(NC(=O)CN4CCCC4)C(O)=C3C(=O)C1=C2O)F)=O.Cl |&1:1,9,13,16,r|
Eravacycline (dihydrochloride) Usage And Synthesis
Uses
Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent.
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].
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. DOI:10.1016/j.ijantimicag.2017.06.022
[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). DOI:10.1128/AAC.00250-17
[3] Xiao XY, et al. Fluorocyclines: a potent, broad spectrum antibacterial agent. J Med Chem. 2012 Jan 26;55(2):597-605. DOI:10.1021/jm201465w
[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. DOI:10.1128/AAC.01288-13
[5] Grossman TH, et al. Eravacycline (TP-434) is efficacious in animal models of infection. Antimicrob Agents Chemother. 2015 May;59(5):2567-71. DOI:10.1128/AAC.04354-14
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