Tigecycline
(Synonyms: 替加环素; GAR-936) 目录号 : GC14574
Tigecycline是第三代四环素类抗生素。
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.
Tigecycline是第三代四环素类抗生素 [1]。Tigecycline与细菌核糖体30S亚基结合，阻断氨酰-tRNA与核糖体A位点的结合，从而抑制蛋白质合成 [2]。Tigecycline素对多种革兰氏阳性菌、革兰氏阴性菌和厌氧菌均具有广谱抗菌活性 [3-4]。
在GAM-016细胞中，Tigecycline（1-10μM；72h）以剂量依赖性方式抑制胃癌细胞增殖 [5]。在AsPC-1细胞中，Tigecycline（1-40μM；72h）以剂量依赖性方式抑制癌细胞增殖 [6]。
在C57BL/6J小鼠中，Tigecycline（0-100mg/kg；ip；5周）有效减少依赖性和非依赖性雌性和雄性小鼠的过量饮酒 [7]。在小鼠脓肿分枝杆菌感染模型中，吸入Tigecycline（0.25-2.50mg；50μL；气雾疗法；4周）对脓肿分枝杆菌具有强效抗菌活性 [8]。
| 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 | |
| 别名 | 替加环素; GAR-936 | ||
| 化学名 | (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 | ||
| 分子式 | C29H39N5O8 | 分子量 | 585.65 |
| 溶解度 | ≥ 29.3mg/mL in DMSO, ≥ 32.47 mg/mL in Water with ultrasonic | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7075 mL | 8.5375 mL | 17.075 mL |
| 5 mM | 0.3415 mL | 1.7075 mL | 3.415 mL |
| 10 mM | 0.1708 mL | 0.8538 mL | 1.7075 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet