Licensed by Pfizer Catalog No.S1403 Synonyms: GAR-936

Tigecycline Chemical Structure

Molecular Weight(MW): 585.65

Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.

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  • CHX blocked Pim-1 AUG isoform translocation from the cytosol to mitochondria and led to reduced pBADS112. Cox-2 was examined to assess the effect of tigecycline on mitochondrial translation. Cy-Cox-2: cytoplasmic Cox-2; Mt-Cox-2: mitochondrial Cox-2.

    Biochem J, 2016, 473(1):99-107. Tigecycline purchased from Selleck.

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Biological Activity

Description Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.
In vitro

Tigecycline evades the Tet(A-E) efflux pumps, which account for most acquired resistance to tetracycline and minocycline in Enterobacteriaceae and Acinetobacter spp. Tigecycline binds to bacterial ribosomes that have been modified by the Tet(M) protein, a mechanism that compromises all available tetracyclines, and which is frequent in Gram-positive cocci and Neisseria spp. Tigecycline remains vulnerable to the chromosomally-encoded multidrug efflux pumps of Proteeae and Pseudomonas aeruginosa, and to Tet(X), a tetracycline-degrading mono-oxygenase found, albeit rarely, in Bacteroides spp. Tigecycline MICs for enterococci, staphylococci, and streptococci are mostly 0.06–0.25 mg/L, again with little or no skew to the distribution. Tigecycline is prone to oxidation, and MIC values, particularly for the most susceptible isolates, may be raised if the drug is added to broth that has become oxygenated during storage, or if drug-containing media are stored before inoculation. [1] Tigecycline is a poor substrate for tetracycline-specific efflux pumps, and it still attaches to ribosomes that have been modified by the Tet(M) protein. Tigecycline has demonstrated activity against a wide variety of gram-positive and gram-negative pathogens, including multidrug-resistant strains. Tigecycline is active against many gram-positive and -negative organisms, including methicillin-resistantStaphylococcus aureus, vancomycin-intermediate and -resistant enterococci, and extended-spectrum β-lactamase–producing Escherichia coli and Klebsiella pneumoniae. Tigecycline exhibits antibacterial activity against a wide spectrum of aerobic and anaerobic bacteria. [2] Tigecycline is a broad-spectrum, protein-inhibiting, antibacterial agent possessing activity against strains resistant to other chemotherapeutic agents. Tigecycline demonstrates in vitro activities against the GISA and the methicillin-resistant and methicillin-susceptible staphylococcal strains tested (MICs at which 90% of isolates tested are inhibited [MIC90s], 0.5 to 1 μg/ml). Tigecycline has MIC90s of 0.25 μg/ml for all of the S. pneumoniae strains and demonstrates similar activities against all of the S. pneumoniae strains tested. [3]

In vivo Tigecycline is bactericidal against methicillin-susceptible S. aureus (MSSA) in the rabbit osteomyelitis model and exhibits good, but not excellent, activity in Legionellapneumophila pneumonia in guinea pigs[1]. Tigecycline at 50 mg/kg twice daily was not toxic to mice. Tigecycline is effective in inhibiting NSCLC growth in vivo through decreasing proliferation and increasing apoptosis of tumor cells[4].


Cell Research:


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  • Cell lines: NSCLC cells
  • Concentrations: 1, 5, 10, 25, 50 μM
  • Incubation Time: 24 h or 3 days
  • Method:

    NSCLC cells were treated with DMSO (as control) or different concentrations of tigecycline for 3 days prior to 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) and apoptosis assays. After 24 h of treatment with tigecycline, cells were harvested for the measurement of mitochondrial functions.

    (Only for Reference)
Animal Research:


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  • Animal Models: SCID mice
  • Formulation: DMSO
  • Dosages: 50 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (170.75 mM)
Water 100 mg/mL (170.75 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 585.65


CAS No. 220620-09-7
Storage powder
in solvent
Synonyms GAR-936

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02931526 Unknown status Bacterial Infection|Critically Ill Zhujiang Hospital August 2016 --
NCT02800785 Recruiting Appendicitis University of Washington|Patient-Centered Outcomes Research Institute May 2016 Not Applicable
NCT01970371 Completed Bloodstream Infections (BSI) Due to CRE|Hospital-Acquired Bacterial Pneumonia (HABP) Due to CRE|Ventilator-Associated Bacterial Pneumonia (VABP) Due to CRE|Complicated Urinary Tract Infection (cUTI) Due to CRE|Acute Pyelonephritis (AP) Due to CRE Achaogen Inc.|Department of Health and Human Services September 16 2014 Phase 3
NCT02040818 Withdrawn Hemodialysis Catheter-related Bacteremia University of California San Diego|National Institutes of Health (NIH) November 2013 Phase 2|Phase 3
NCT01789905 Completed Intra-Abdominal Infections|Skin Disease Infectious Pfizer April 15 2013 --
NCT01721408 Completed Intra-abdominal Infection Pfizer November 2012 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID