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替加环素

糖基环素抗生素
规格或纯度: ≥96%
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货号 (SKU) 包装规格 是否现货 价格 数量
E129449-10mg 10mg 现货 Stock Image
E129449-50mg 50mg 现货 Stock Image
E129449-250mg 250mg 现货 Stock Image
E129449-1g 1g 现货 Stock Image
E129449-5g 5g 现货 Stock Image
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四环素类 四环素类抗生素

基本描述

规格或纯度 ≥96%
英文名称 Tigecycline
别名 9-叔丁基甘氨酰氨基米诺环素,替加环素
英文别名 9-t-Butylglycylamido-minocycline; TBG-MINO; Tigecyclin; Tygacil;(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;9-tert-Butylglycylamidomino
生化机理 Tigecycline 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.Glycylcycline antibiotic. Active against Gram-negative and Gram-positive bacteria. Active in vivo. Active against multi-drug resistant pathogens.
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

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。

Tigecycline is a broad spectrum glycylcycline antibiotic. Tigecycline is bacteriostatic. It inhibits protein synthesis through 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.
A broad spectrum glycylcycline antibiotic

名称和标识符

IUPAC 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
INCHI InChI=1S/C29H39N5O8/c1-28(2,3)31-11-17(35)32-15-10-16(33(4)5)13-8-12-9-14-21(34(6)7)24(38)20(27(30)41)26(40)29(14,42)25(39)18(12)23(37)19(13)22(15)36/h10,12,14,21,31,36-37,40,42H,8-9,11H2,1-7H3,(H2,30,41)(H,32,35)/t12-,14-,21-,29-/m0/s1
InChi Key SOVUOXKZCCAWOJ-HJYUBDRYSA-N
Canonical SMILES CC(C)(C)NCC(=O)NC1=CC(=C2CC3CC4C(C(=O)C(=C(C4(C(=O)C3=C(C2=C1O)O)O)O)C(=O)N)N(C)C)N(C)C
分子式

C29H39N5O8

PubChem CID 54686904
分子量 585.65

化学和物理性质

溶解性 DMSO 100 mg/mL Water 100 mg/mL Ethanol <1 mg/mL
敏感性 对热敏感
熔点 185 °C(dec.)
比旋光度 -199° (C=0.15,CH3OH)

安全信息

象形图
ghs08

Health Hazard

ghs09

Environmental Hazard

ghs07

Harmful

信号词 Danger
危险声明 H319: Causes serious eye irritation
H411: Toxic to aquatic life with long lasting effects
H360: May damage fertility or the unborn child
预防措施声明 P305+P351+P338,P273,P280,P405,P501,P391,P203,P264+P265,P318,P337+P317
Merck Index 9432

关联配体

Ligand ID 10929
名称 tigecycline
别名 Tygacil®
类别 Synthetic organic
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
生物活性评价 MIC data is available in these references:
评价 Sulfadimidine (sulfamethazine) is a sulfonamide antibacterial compound. This class of compounds are competitive inhibitors of bacterial dihydropteroate synthase (DHPS), an enzyme in the pathway which generates the folic acid that is essential for bacterial growth.

参考文献

1. Bhavnani SM, Rubino CM, Ambrose PG, Babinchak TJ, Korth-Bradley JM, Drusano GL.  (2010)  Impact of different factors on the probability of clinical response in tigecycline-treated patients with intra-abdominal infections..  Antimicrob Agents Chemother,  54  (3):  (1207-12).  [PMID:20038623]
2. Hajdu S, Holinka J, Reichmann S, Hirschl AM, Graninger W, Presterl E.  (2010)  Increased temperature enhances the antimicrobial effects of daptomycin, vancomycin, tigecycline, fosfomycin, and cefamandole on staphylococcal biofilms..  Antimicrob Agents Chemother,  54  (10):  (4078-84).  [PMID:20679509]
3. Cercenado E, Marín M, Sánchez-Martínez M, Cuevas O, Martínez-Alarcón J, Bouza E.  (2007)  In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods..  Antimicrob Agents Chemother,  51  (3):  (1102-4).  [PMID:17194827]

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