Tigecycline (GAR-936)

Licensed by Pfizer Catalog No.S1403

For research use only.

Tigecycline (GAR-936) 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 (GAR-936) Chemical Structure

CAS No. 220620-09-7

Selleck's Tigecycline (GAR-936) has been cited by 10 Publications

1 Customer Review

Purity & Quality Control

Choose Selective Antineoplastic and Immunosuppressive Antibiotics Inhibitors

Biological Activity

Description Tigecycline (GAR-936) 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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP-1 NXP4ZpVbSW62aXLhZ5RmemmjbDDhd5NigQ>? M4r3cFI1KGi{cx?= NYqwOYFsSW62aXLhZ5RmemmjbDDhZ5Rqfmm2eTDh[4FqdnO2IGP0ZZBpgWyxY3;jZ5V{KGG3cnX1d{BUS1ZiaYPvcIF1\WRiZoLvcUBkgXO2aXOg[oljem:|aYOgdIF1cWWwdDDpcoZm[3SnZDDpckBpfW2jbjDUTHAuOSClZXzsd{Bie3Onc4Pl[EBieyCub3egdoVlfWO2aX;uJI9nKGmwdILhZ4VtdHWuYYKgR2ZWKGyndnXsJIFnfGW{IEK0JIhzeyCrbjDwdoV{\W6lZTDv[kB1cHmvaXTpcoU> NUjlXFNoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxPFg{QTNpPkG5NVg5Ozl|PD;hQi=>
Assay
Methods Test Index PMID
Western blot Cyclin D1 / CDK2 / p21 ; p62 / LC3-I / LC3-II ; p-AMPKα / AMPKα / p-mTOR / mTOR / p-p70S6K / p70S6K / p-4E-BP-1 / 4E-BP1 ; Cox-1 / Cox-2 / Cox-4 ; CDK2 / Cyclin E ; E-cadherin / Vimentin 30247801 30082885 26621850
Growth inhibition assay Cell viability 30247801
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].

Protocol (from reference)

Cell Research:

[4]

  • 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.

Animal Research:

[4]

  • Animal Models: SCID mice
  • Dosages: 50 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 585.65
Formula

C29H39N5O8

CAS No. 220620-09-7
Storage 3 years -20°C powder
2 years -80°C in solvent
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

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04937894 Recruiting Drug: Tigecycline Infectious Disease Shandong University|Shandong Provincial Hospital June 1 2021 --
NCT04724798 Recruiting -- Extracorporeal Membrane Oxygenation|Pharmacokinetics|Tigecycline Nanfang Hospital of Southern Medical University January 20 2020 --
NCT04489459 Unknown status Drug: Colistin|Drug: Meropenem|Drug: Tigecycline Treatment of Blood Stream Infections Due to Multidrug-Resistant Klebsiella Pneumoniae Al-Azhar University September 21 2019 Phase 4
NCT03034174 Unknown status -- Septic Shock|Antibiotic Resistant Infection|Critical Illness Medical University of Lublin January 15 2017 --
NCT02883036 Unknown status Other: blood sampling Chronic Myeloid Leukemia Nanfang Hospital of Southern Medical University September 2016 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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