For research use only.
Licensed by Pfizer Catalog No.S1403 Synonyms: GAR-936
CAS No. 220620-09-7
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.
Selleck's Tigecycline has been cited by 8 publications
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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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|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.|
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.  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.  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. 
|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. 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.|
|In vitro||DMSO||100 mg/mL (170.75 mM)|
|Water||100 mg/mL (170.75 mM)|
|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.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04489459||Recruiting||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||Not yet recruiting||Other: blood sampling||Chronic Myeloid Leukemia||Nanfang Hospital of Southern Medical University||September 2016||--|
|NCT02931526||Unknown status||Drug: Tigecycline||Bacterial Infection|Critically Ill||Zhujiang Hospital||August 2016||--|
|NCT01840319||Completed||--||Survival Status at Day 30 After the Last Intake||Pfizer||February 2013||--|
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.
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