Home Microbiology Antineoplastic and Immunosuppressive Antibiotics inhibitor - Bacterial chemical - Autophagy activator Tigecycline For research use only.

Tigecycline

Synonyms: GAR-936, WAY-GAR-936, TBG-MINO

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. Tigecycline induces autophagy by downregulating the PI3K-AKT-mTOR pathway.

Tigecycline Chemical Structure

Tigecycline Chemical Structure

CAS No. 220620-09-7

Purity & Quality Control

Tigecycline Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP-1 Antibacterial assay 24 hrs Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level after 24 hrs in presence of thymidine 19188393
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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. Tigecycline induces autophagy by downregulating the PI3K-AKT-mTOR pathway.
In vitro
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]
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot E-cadherin / Vimentin CDK2 / Cyclin E Cox-1 / Cox-2 / Cox-4 p-AMPKα / AMPKα / p-mTOR / mTOR / p-p70S6K / p70S6K / p-4E-BP-1 / 4E-BP1 p62 / LC3-I / LC3-II Cyclin D1 / CDK2 / p21 26621850
Growth inhibition assay Cell viability 30247801
In Vivo
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].
Animal Research Animal Models SCID mice
Dosages 50 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06049771 Recruiting
Carbapenem-resistant Enterobacteriaceae
Phramongkutklao College of Medicine and Hospital|Silpakorn University
 September 17 2023 Not Applicable
NCT05698160 Not yet recruiting
Blood Coagulation Disorder
The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School
 May 1 2023 --
NCT04937894 Recruiting
Infectious Disease
Shandong University|Shandong Provincial Hospital
 June 1 2021 --
NCT04724798 Unknown status
Extracorporeal Membrane Oxygenation|Pharmacokinetics|Tigecycline
Nanfang Hospital Southern Medical University
 January 20 2020 --
NCT04489459 Unknown status
Treatment of Blood Stream Infections Due to Multidrug-Resistant Klebsiella Pneumoniae
Al-Azhar University
 September 21 2019 Phase 4

Chemical Information & Solubility

Molecular Weight 585.65 Formula

C29H39N5O8
CAS No. 220620-09-7 SDF Download Tigecycline SDF
Smiles CC(C)(C)NCC(=O)NC1=CC(=C2CC3CC4C(C(=O)C(=C(C4(C(=O)C3=C(C2=C1O)O)O)O)C(=O)N)N(C)C)N(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (170.75 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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