Tigecycline (Synonyms: GAR 936, Glycylcycline) |
Katalog-Nr.GC14574
One-Click Copy Product Info
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Tigecyclin (GAR-936) ist ein Breitband-Glycylcyclin-Antibiotikum.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 220620-09-7
Sample solution is provided at 25 µL, 10mM.
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Tigecycline is a third-generation tetracycline-derived antibiotic [1]. Tigecycline binds to the bacterial 30S ribosomal subunit, blocking aminoacyl-tRNA binding to the ribosomal A site, thereby inhibiting protein synthesis [2]. Tigecycline exhibits broad-spectrum antibacterial activity against a variety of Gram-positive, Gram-negative, and anaerobic bacteria [3-4].
In GAM-016 cells, Tigecycline (1-10μM; 72h) inhibits the proliferation of gastric cancer cells in a dose-dependent manner [5]. In AsPC-1 cells, Tigecycline (1-40μM; 72h) inhibits the proliferation of cancer cells in a dose-dependent manner [6].
In C57BL/6J mice, Tigecycline (0-100mg/kg; ip; 5 weeks) effectively reduces excessive alcohol consumption in dependent and nondependent female and male mice [7]. In M. abscessus infection mouse model, inhaled Tigecycline (0.25-2.50mg; 50μL; aerosol therapy; 4 weeks) has potent antibacterial activity against M. abscessus [8].
References:
[1]. Rose W E, Rybak M J. Tigecycline: first of a new class of antimicrobial agents[J]. Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, 2006, 26(8): 1099-1110.
[2]. Anandabaskar N. Protein synthesis inhibitors[M]//Introduction to basics of pharmacology and toxicology: volume 2: essentials of systemic pharmacology: from principles to practice. Singapore: Springer Nature Singapore, 2021: 835-868.
[3]. Slover C M, Rodvold K A, Danziger L H. Tigecycline: a novel broad-spectrum antimicrobial[J]. Annals of Pharmacotherapy, 2007, 41(6): 965-972.
[4]. Yaghoubi S, Zekiy A O, Krutova M, et al. Tigecycline antibacterial activity, clinical effectiveness, and mechanisms and epidemiology of resistance: narrative review[J]. European Journal of Clinical Microbiology & Infectious Diseases, 2022, 41(7): 1003-1022.
[5]. Tang C, Yang L, Jiang X, et al. Antibiotic drug tigecycline inhibited cell proliferation and induced autophagy in gastric cancer cells[J]. Biochemical and biophysical research communications, 2014, 446(1): 105-112.
[6]. Yang J, Dong Z, Ren A, et al. Antibiotic tigecycline inhibits cell proliferation, migration and invasion via down‐regulating CCNE2 in pancreatic ductal adenocarcinoma[J]. Journal of cellular and molecular medicine, 2020, 24(7): 4245-4260.
[7]. Bergeson S E, Nipper M A, Jensen J, et al. Tigecycline Reduces Ethanol Intake in Dependent and Nondependent Male and Female C57 BL/6J Mice[J]. Alcoholism: Clinical and Experimental Research, 2016, 40(12): 2491-2498.
[8]. Pearce C, Ruth M M, Pennings L J, et al. Inhaled tigecycline is effective against Mycobacterium abscessus in vitro and in vivo[J]. Journal of Antimicrobial Chemotherapy, 2020, 75(7): 1889-1894.
| Cell experiment [1]: | |
Cell lines | GAM-016 cells |
Preparation Method | Tigecycline was dissolved in Dimethyl Sulfoxide (DMSO) as 100mM stock solutions. Primary gastric cancer cells were treated with Tigecycline (1μM, 5μM, 10μM) or DMSO for 72h. Micrographs of cell morphology were taken by an Olympus microscopy. Cell survival was analyzed by Trypan blue exclusion assay. |
Reaction Conditions | 1-10μM; 72h |
Applications | Tigecycline inhibits the proliferation of gastric cancer cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Tigecycline was prepared at doses of 0, 40, 60, 80, and 100mg/kg in sterile saline (0.9% NaCl) and used within 25 hours at 0.01mL/g body weight. The ability of Tigecycline to decrease 15E intake in dependent (CIE) and nondependent (control) male and female mice was tested after 4 cycles of CIE vapor or control air exposure, using a within-subjects design. Doses were administered intraperitoneally and in random order to all mice, with a 1-hour pretreatment time. Baseline 15E intake was re-established prior to administration of subsequent injections. |
Dosage form | 0-100mg/kg; ip; 5 weeks |
Applications | Tigecycline effectively reduces excessive alcohol consumption in dependent and nondependent female and male mice. |
References: | |
| Cas No. | 220620-09-7 | SDF | |
| Überlieferungen | GAR 936, Glycylcycline | ||
| Chemical Name | (4S,4aS,5aR,12aR)-9-[[2-(tert-butylamino)acetyl]amino]-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide | ||
| Canonical SMILES | CC(C)(C)NCC(=O)NC1=C(C2=C(CC3CC4C(C(=O)C(=C(C4(C(=O)C3=C2O)O)O)C(=O)N)N(C)C)C(=C1)N(C)C)O | ||
| Formula | C29H39N5O8 | M.Wt | 585.65 |
| Löslichkeit | ≥ 29.3mg/mL in DMSO, ≥ 32.47 mg/mL in Water with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7075 mL | 8.5375 mL | 17.075 mL |
| 5 mM | 341.5 μL | 1.7075 mL | 3.415 mL |
| 10 mM | 170.8 μL | 853.8 μL | 1.7075 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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 saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)