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TP-6076

Names

[ CAS No. ]:
1575495-01-0

[ Name ]:
TP-6076

Biological Activity

[Description]:

TP-6076 is a fully synthetic fluorocycline antibiotic, acts function via binding to the 30S ribosomal subunit and maintains its activity. TP-6076 displays potent mechanism-based antitranslational activity (Tet protein, IC50=0.18 μg/mL), shows a wide range of antimicrobial and antiparasitic activities[1][2].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Bacterial

[In Vitro]

TP-271 (0.01 ng/mL-100 μg/mL; 72 h) is active in MIC assays against key community respiratory Gram-positive and Gram-negative pathogens[2]. Cell Viability Assay[2] Cell Line: Streptococcus pneumoniae, Staphylococcus aureus, S. aureus, Streptococcus pyogenes, Haemophilus influenzae, and Moraxella catarrhalis Concentration: 0.01 ng/mL-100 μg/mL Incubation Time: 72 hours Result: Inhibited the growth of Streptococcus pneumoniae (MIC90=0.03 µg/mL), methicillin-sensitive Staphylococcus aureus (MSSA; MIC90=0.25 µg/mL), methicillin-resistant S. aureus (MRSA; MIC90=0.12 µg/mL), Streptococcus pyogenes (MIC90= 0.03 µg/mL), Haemophilus influenzae (MIC90=0.12 µg/mL), and Moraxella catarrhalis (MIC90≤0.016 µg/mL).

[In Vivo]

TP-6076 reduces the bacterial burden in the lung in murine pneumonia models with MRSA, S. pneumoniae, and H. influenzae (1, 5, and 10 mg/kg for i.v.; 12.5, 25, 50 mg/kg for p.o.; single dose), neutropenic murine S. pneumoniae tet(M) pneumonia model (1, 5, and 10 mg/kg for i.v.; 0.3, 3, 10 mg/kg for p.o.; single dose), and immunocompetent mouse S. pneumoniae pneumonia model (30 mg/kg for p.o.; single dose)[2].

Chemical & Physical Properties

[ Molecular Formula ]:
C28H32F3N3O7

[ Molecular Weight ]:
579.56


Related Compounds

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