Tigecycline

Catalog No.S1403 Batch:S140350

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Technical Data

Formula

C29H39N5O8

Molecular Weight 585.65 CAS No. 220620-09-7
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)
Clear solution
Saline
30.0mg/ml Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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].

Protocol (from reference)

Cell Assay:

[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 Study:

[4]

  • Animal Models

    SCID mice

  • Dosages

    50 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Biochem J, 2016, 473(1):99-107]

Selleck's Tigecycline has been cited by 14 publications

Tigecycline Opposes Bortezomib Effect on Myeloma Cells Decreasing Mitochondrial Reactive Oxygen Species Production [ Int J Mol Sci, 2024, 25(9)4887] PubMed: 38732105
Tigecycline Opposes Bortezomib Effect on Myeloma Cells Decreasing Mitochondrial Reactive Oxygen Species Production [ Int J Mol Sci, 2024, 25(9)4887] PubMed: 38732105
Meropenem-ANT3310, a unique β-lactam-β-lactamase inhibitor combination with expanded antibacterial spectrum against Gram-negative pathogens including carbapenem-resistant Acinetobacter baumannii [ Antimicrob Agents Chemother, 2024, 68(3):e0112023] PubMed: 38289044
Sustained activation of EGFR-ERK1/2 signaling limits the response to tigecycline-induced mitochondrial respiratory deficiency in liver cancer [ EBioMedicine, 2022, 87:104397] PubMed: 36502574
Activity of Drug Combinations against Mycobacterium abscessus Grown in Aerobic and Hypoxic Conditions [ Microorganisms, 2022, 10(7)1421] PubMed: 35889140
The long non-coding RNA CDK6-AS1 overexpression impacts on acute myeloid leukemia differentiation and mitochondrial dynamics [ iScience, 2021, 24(11):103350] PubMed: 34816103
Targeting Mitochondria in Melanoma [ Biomolecules, 2020, 10(10)E1395] PubMed: 33007949
Sirt1 gene confers Adriamycin resistance in DLBCL via activating the PCG-1α mitochondrial metabolic pathway [ Aging (Albany NY), 2020, 12(12):11364-11385] PubMed: 32570218
BRCA1 Deficiency Upregulates NNMT, Which Reprograms Metabolism and Sensitizes Ovarian Cancer Cells to Mitochondrial Metabolic Targeting Agents [ Cancer Res, 2019, 79(23):5920-5929] PubMed: 31619387
Tigecycline as a dual inhibitor of retinoblastoma and angiogenesis via inducing mitochondrial dysfunctions and oxidative damage. [ Sci Rep, 2018, 8(1):11747] PubMed: 30082885

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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