计算溶液所需的质量、体积或浓度。
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 22 篇同行评审文献引用。
概述
Tigecycline is a broad spectrum glycylcycline antibiotic. Tigecycline is bacteriostatic. It inhibits protein synthesis throμgh the binding of the 30S ribosomal subunit of bacteria. This blocks entry of Aminoacyl-tRNA into the A site of the ribosome during translation. Tigecycline is active against resistant strains of gram-positive and gram-negative bacteria, avoiding the two most common mechanisms of resistance to the tetracycline antimicrobials: tetracycline efflux pump proteins and ribosomal protection proteins.Tigecycline 是一种广谱的甘氨酰环素抗生素,对 E. coli (MG1655 菌株) 的平均抑制浓度 (MIC) 约为 125 ng/ mL。对 Acinetobacter baumannii (A. baumannii) 的 MIC50 和 MIC90 分别为 1 和 2 mg/L。
Information
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 induc
In vitro
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\xa0Escherichia coli\xa0and\xa0Klebsiella pneumoniae.\xa0Tigecycline 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.
Cell Data
cell lines：HCT116, HCA7, Caco2 and NCI-H716 cells
Concentrations：1, 5, 10, 25, 50 μM
Incubation Time：24 h or 3 days
Powder Purity:≥96%
规格
英文别名
(4S,4aS,5aR,12aS)-9-(2-(tert-butylamino)acetamido)-4,7-bis(dimethylamino)-3,10,12,12a-tetrahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Tigecycline (GAR-936)
生化机理
替加环素（GAR-936）具有抑菌作用，是一种蛋白质合成抑制剂，能与细菌的 30S 核糖体亚基结合，从而阻止 Aminoacyl-tRNA 在原核生物翻译过程中进入核糖体的 A 位点。替加环素通过下调 PI3K-AKT-mTOR 通路诱导自噬。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
细菌 70S 核糖体抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)(C)NCC(=O)NC1=CC(=C2C[C@H]3C[C@H]4[C@@H](C(=O)C(=C([C@]4(C(=O)C3=C(C2=C1O)O)O)O)C(=O)N)N(C)C)N(C)C
分子量
585.65
Reaxy-Rn
35955618
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=35955618&ln=
技术文档
高级数据
产品属性
| ALogP | 1.1 |
|---|
化学和物理性质
比旋光度
-199° (C=0.15,CH3OH)
熔点
185 °C(dec.)
安全和危险性（GHS）
信号词
Danger
危险声明
H319: 引起严重眼睛刺激
H411: 对水生生物有毒并具有长期持续影响
H360: 可能损害生育力或未出生的孩子
预防措施声明
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
P273: 避免释放到环境中。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P405: 密闭存放
P501: 将内容物/容器处理到。。。
P391: 收集溢出物
P203: 使用前，获取、阅读并遵守所有安全说明。
P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。
P318: 如果暴露或担心，请就医。
P337+P317: 如果眼睛刺激持续：寻求医疗帮助。
Merck Index
9432
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 L2230018 |
分析证书 | T409266 |
技术文档和文章
此产品的引用文献
溶液计算器
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