TIGECYCLINE GLYCYLCYCLINE
Tigecycline
CAS: 220620-09-7
Molecular Formula: C29H39N5O8
TIGECYCLINE GLYCYLCYCLINE - Names and Identifiers
TIGECYCLINE GLYCYLCYCLINE - Physico-chemical Properties
| 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. |
TIGECYCLINE GLYCYLCYCLINE - Risk and Safety
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| UN IDs | 3077 |
| RTECS | QI7619500 |
| HS Code | 29419090 |
| Hazard Class | 9 |
| Packing Group | III |
TIGECYCLINE GLYCYLCYCLINE - Reference
| 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 |
TIGECYCLINE GLYCYLCYCLINE - Reference Information
| introduction | tigecycline is a broad-spectrum glycyl tetracycline antibacterial drug, which widely covers G cocci, G-bacilli, MRSA, ESBLS positive Enterobacter, Stenotrophomonas maltophilia and multidrug resistant Acinetobacter baumannii. |
| use | tigecycline is used to treat infections of drug-resistant bacteria such as staph aureus and acinetobacter baumannii. |
| Glycylcycline antibiotics | Tigecycline, also known as 9-tert-butylglycylamino minocycline or butylminocycline, is a new type of broad-spectrum active intravenous antibiotic, belonging to 9-tert-butylglycylamide minocycline derivative, is the first glycylcycline antibiotic, it was developed to solve the early tetracycline resistance and was approved by the US FDA in June 1995. Although its structure is similar to minocycline, after the molecular structure is changed, not only its antibacterial activity is greatly improved, but also compared with other tetracycline drugs, bacteria are not easy to develop resistance to it, and it is resistant to methicillin-resistant Staphylococcus aureus is also active. The mechanism of action of tigecycline is similar to that of tetracycline antibiotics. It prevents the entry of transfer RNA by combining with the 30S ribosome of bacteria, making it impossible for amino acids to combine into peptide chains, and ultimately blocking bacterial protein synthesis, The role of restricting bacterial growth. But the binding ability of tigecycline to ribosomes is 5 times that of other tetracycline drugs. This shows that the ability of this product to resist bacterial resistance is better than other tetracycline drugs. The antibacterial spectrum of tigecycline includes gram-positive bacteria, gram-negative bacteria and anaerobic bacteria. In vitro experiments and clinical trials show that, tigecycline is sensitive to some aerobic Gram-negative bacteria (such as Citrobacter freund, Enterobacter cloacae, Escherichia coli, Klebsiella acid-producing bacteria and Klebsiella pneumoniae, Acinetobacter baumannii, Hydrovapophilus, Citrobacter crenelii, Enterobacter aerogenes, Pasteuria hemorrhagic sepsis, Serratia marcescens and Stenotrophomonas maltophilia, etc.). Pseudomonas aeruginosa is resistant to tigecycline. |
| indications | tigecycline can be used as a choice after failure of first-line drug treatment for multidrug-resistant bacteria, and it is also a new treatment option for patients who are allergic to penicillin or cannot tolerate other drug treatment. It is used for the treatment of patients aged 18 and above with complex skin and skin structure infection or complex intra-abdominal infection, including complex appendicitis, burn infection, intra-abdominal abscess, deep soft tissue infection and ulcer infection. |
| adverse reactions | in clinical trials, the most common adverse events caused by tigecycline are nausea and vomiting, which usually occur within the first 1~2 days of treatment, and the degree is mostly mild to moderate. In positive drug-controlled clinical trials, the incidence of nausea and vomiting in patients with complex skin and skin structure infections was 35% and 20% respectively when treated with tigecycline. The incidence of nausea and vomiting were 8.9% and 4.2% respectively when treated with vancomycin/aztreonam. The incidence of nausea and vomiting in patients with complex intra-abdominal infection treated with tigecycline was 25.3% and 19.5% respectively. The incidence of nausea and vomiting were 20.5% and 15.3% respectively when treated with vancomycin/aztreonam. |
| Biological activity | Tigecycline (GAR-936) is a glycyl cyclin antibiotic, which has antibacterial effect and is an inhibitor of protein synthesis. The 30S ribosomal subunit binds to prevent the aminoacyl tRNA from entering the site of the ribosome during prokaryotic translation. Tigecycline can induce autophagy by down-regulating PI3K-AKT-mTOR pathway. |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 15:16:48
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View History
TIGECYCLINE GLYCYLCYCLINE
4-((difluoromethyl)thio)aniline HCl
癸硼烷(14)
Chromate(2-), [2,4-dihydro-4-[(2-hydroxy-5-nitrophenyl)azo]-5-methyl-2-phenyl-3H-pyrazol-3-onato(2-)][3-[(4,5-dihydro-3-methyl-5-oxo-1-phenyl-1H-pyrazol-4-yl)azo]-2-hydroxy-5-nitrobenzenesulfonato(3-)]-, disodium
preparation 1311
甲基(2-甲基-3-呋喃基)二硫
Einecs 281-527-5
3-氟-5-硝基苯三氟甲基3-氟-5-三氟甲基硝基苯
METOCLOPRAMIDE HYDROCHLORIDE, MONOHYDRATE
2-(4-氟苯氧基)-1-乙胺盐酸盐
4-((difluoromethyl)thio)aniline HCl
癸硼烷(14)
Chromate(2-), [2,4-dihydro-4-[(2-hydroxy-5-nitrophenyl)azo]-5-methyl-2-phenyl-3H-pyrazol-3-onato(2-)][3-[(4,5-dihydro-3-methyl-5-oxo-1-phenyl-1H-pyrazol-4-yl)azo]-2-hydroxy-5-nitrobenzenesulfonato(3-)]-, disodium
preparation 1311
甲基(2-甲基-3-呋喃基)二硫
Einecs 281-527-5
3-氟-5-硝基苯三氟甲基3-氟-5-三氟甲基硝基苯
METOCLOPRAMIDE HYDROCHLORIDE, MONOHYDRATE
2-(4-氟苯氧基)-1-乙胺盐酸盐