Eravacycline dihydrochloride is a potent and broad-spectrum antibacterial agent.

Eravacycline shows inhibitory effects on six E. coli with MICs ranging from 0.125 to 0.25 mg/L.?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.?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.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.

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.

1334714-66-7

C27H33Cl2FN4O8

631.48

TP-434 dihydrochloride;TP-434-046

DMSO:150 mg/mL (237.54 mM),Need ultrasonic
H2O:50 mg/mL (79.18 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years