Molecular Formula | C29H39N5O8 |
Molar Mass | 585.65 |
Density | 1.45±0.1 g/cm3(Predicted) |
Melting Point | 164-166°C |
Boling Point | 890.9±65.0 °C(Predicted) |
Flash Point | 492.612°C |
Solubility | DMSO 100 mg/ml |
Vapor Presure | 0mmHg at 25°C |
Appearance | Orange powder |
Color | Orange |
Merck | 14,9432 |
pKa | 4.50±1.00(Predicted) |
Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
Refractive Index | 1.675 |
MDL | MFCD00935753 |
In vitro study | Tigecycline avoids the Tet(A-E) efflux pump, which is responsible for the acquired resistance of most Enterobacteriaceae and Acinetobacter to tetracycline and A- E. Bacterial ribosomes modified with Tet(M) proteins, usually in Gram-positive cocci and Neisseria gonorrhoeae, render all available antibiotics ineffective, and Tigecycline is able to bind to it without being ineffective. Tigecycline is still vulnerable to attack by the Proteobacteria and the chromosome-encoded multidrug efflux pump of Pseudomonas aeruginosa, and is also subject to Tet(X), found in the genus Bacteroides, although rarely degraded by a tetracycline, monooxygenase attacks. The MICs of Tigecycline against Enterococci, staphylococci, and Streptococci are mostly 0.06-0.25 mg/L, and the distribution pattern is almost not oblique. Tigecycline is easily oxidized. If a drug that has been oxidized during storage is added to a liquid medium, or a medium containing a drug is stored before inoculation, the MIC value of Tigecycline, especially the most sensitive strain, it may improve. Tigecycline is a poor substrate for the tetracycline-specific efflux pump, and it adheres to bacterial ribosomes modified with Tet(M) protein. Tigecycline is active against a variety of gram-positive and gram-negative pathogens, including multidrug-resistant strains. Tigecycline is effective against many Gram-positive and gram-negative organisms, including methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci, and extended-spectrum beta-lactamase-resistant Escherichia Coli and Klebsiella pneumoniae. Tigecycline has broad-spectrum antibacterial activity against aerobic and anaerobic bacteria. Tigecycline is a broad-spectrum protein-inhibiting antibacterial agent that is resistant to other antibiotic-resistant strains. In vitro tests, tests of methicillin-resistant and methicillin-sensitive Staphylococcus aureus strains showed that Tigecycline had anti-GISA activity (MICs ,90% of in vitro test strains were inhibited [MIC90s],0.5 -1 μg/ml). Tigecycline had a MIC90 s of 0.25 μg/ml against all S. Pneumoniae strains and had similar activity against all S. Pneumoniae strains tested. |
In vivo study | In a rabbit model with osteomyelitis, Tigecycline as an antibacterial agent was able to resist methicillin-resistant Staphylococcus aureus (MSSA), and in guinea pigs with Legionella pneumophila pneumonia, it was able to exert good, but not excellent activity. The frequency of administration of 50 mg/kg Tigecycline twice daily had no toxic effect on mice. Tigecycline is effective in inhibiting the growth of NSCLC in vivo, mainly by reducing the proliferation of tumor cells and increasing their apoptosis. |
Safety Description | 24/25 - Avoid contact with skin and eyes. |
UN IDs | 3077 |
RTECS | QI7619500 |
HS Code | 29419090 |
Hazard Class | 9 |
Packing Group | III |
Reference Show more | 1. Ma Lin, Sun Jialin, Li Enze et al. Simultaneous Determination of Voriconazole and tigecycline in Human Plasma by LC-MS/MS [J]. Chinese Journal of Clinical Pharmacology 2019 035(024):3237-3240. 2. [IF = 4.003] Hui Zhang et al. in vitro and in vivo Activity of Combinations of Polymyxin B with other Antimicrobials Against Carbapenem-Resistant Acinetobacter baumannii.Infect Drug Resist.2021 Nov;14:4657-4666 3. [IF = 5.882] Zi-Jian Zheng et al."MALDI-TOF MS for rapid detection and differentiation between Tet(X)-producers and non-Tet(X)-producing tetracycline-resistant Gram-negative bacteria." Virulence. 2022;13(1):77-88 |