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Tigecycline

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Catalog No.
A5226
甘氨环素抗生素
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 950.00
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5mg
¥ 500.00
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25mg
¥ 1,200.00
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100mg
¥ 3,420.00
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Background

Tigecycline, the first commercially available member of the glycylcyclines, is a new class of antimicrobial agents.

The glycylcyclines are the derivatives of tetracycline antibiotics, with modifications in the structure showing potent activity against gram-positive, gram-negative, and certain multidrug-resistant strains [1]. Tigecyclineis bacteriostatic could reversibly bind to the 30S ribosomal subunit thus inhibiting protein translation [1].

In vitro:Tigecycline exihibited good in vitro activities. The range of MIC90s was 0.12-0.5 μg/ml for vancomycin-susceptible and -resistant strains of Enterococcus faecalis and Enterococcus faecium [2]. Tigecyclinewas concentrated in cells and eliminated primarily via biliary excretion. Diminished renal function didn’t significantly alter its systemic clearance. Tigecycline didn’t interfere with common cytochrome P450 enzymes, making pharmacokinetic drug interactions uncommon [3].The tissue penetration of tigecycline was excellent and the compound showed equivalence to imipenem/cilastatin in intra-abdominal infection and to vancomycin plus aztreonam in skin and skin structure infection [4].

In vivo: In an intraperitoneal systemic murine infection model, tigecycline exihibited in vivo activities against GISA, methicillin-susceptible S. aureus and methicillin-resistant S. aureus strains [2]. Tigecycline and daptomycin showed similar in vivo efficacies against infections caused by the MSSA strain (strain GC 4543) with the ED50s of 0.12 and 0.24 mg/kg, respectively. The ED50s of tigecycline was 0.72 mg/kg [2].

Clinical trials: For complicated skin and skin-structure infections in hospitalized patients receiving tigecycline (50-mg, q12h), the microbial eradication rates and clinical cure rates were 70% and 74%. In patients who received 25-mg doses, the results were 56% and 67% [5]. Adverse events including increased nausea and vomiting appeared in treating patients with cSSSI. Tigecycline monotherapy was as safe and efficacious as the vancomycin-aztreonam combination in treating patients with cSSSI[6].

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] Petersen P J, Bradford P A, Weiss W J, et al.  In vitro and in vivo activities of tigecycline (GAR-936), daptomycin, and comparative antimicrobial agents against glycopeptide-intermediate Staphylococcus aureus and other resistant gram-positive pathogens[J]. Antimicrobial agents and chemotherapy, 2002, 46(8): 2595-2601.
[3] Stein G E, Craig W A.  Tigecycline: a critical analysis[J]. Clinical infectious diseases, 2006, 43(4): 518-524.
[4] Livermore D M.  Tigecycline: what is it, and where should it be used[J]. Journal of Antimicrobial Chemotherapy, 2005, 56(4): 611-614.
[5] Postier R G, Green S L, Klein S R, et al.  Results of a multicenter, randomized, open-label efficacy and safety study of two doses of tigecycline for complicated skin and skin-structure infections in hospitalized patients[J]. Clinical therapeutics, 2004, 26(5): 704-714.
[6] Grosse E J E, Babinchak T, Dartois N, et al.  The efficacy and safety of tigecycline in the treatment of skin and skin-structure infections: results of 2 double-blind phase 3 comparison studies with vancomycin-aztreonam[J]. Clinical infectious diseases, 2005, 41(Supplement 5): S341-S353.

文献引用

1. Martin TD, Cook DR, et al. "A Role for Mitochondrial Translation in Promotion of Viability in K-Ras Mutant Cells." Cell Rep. 2017 Jul 11;20(2):427-438. PMID:28700943

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt585.65
Cas No.220620-09-7
FormulaC29H39N5O8
Solubility≥29.3mg/mL in DMSO, <2.53 mg/mL in EtOH, ≥32.47 mg/mL in H2O with ultrasonic
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
SDFDownload SDF
Canonical SMILESCC(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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

抗菌药敏试验 [1]:

细菌

耐药以及敏感革兰氏阳性菌株

制备方法

在DMSO中的溶解度大于29.3 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

18 ~ 22小时

实验结果

Tigecycline对GISA葡萄球菌、耐Methicillin葡萄球菌和Methicillin敏感葡萄球菌显示出类似的体外活性 (MIC90 = 0.5 ~ 1 μg/mL)。此外,Tigecycline还对Vancomycin敏感的和耐Vancomycin的粪肠球菌和屎肠球菌显示出良好的体外活性,其MIC90值为0.12 ~ 0.5 μg/mL。

动物实验 [1]:

动物模型

通过腹腔注射细菌制作的小鼠全身感染模型

给药剂量

0.2 mL,0.01 M;静脉注射;单剂量

实验结果

对于由MSSA菌株引起的感染,Daptomycin和Tigecycline显示出类似的体内作用,其ED50值分别为0.12 mg/kg和0.24 mg/kg。此外,Tigecycline和Daptomycin对于由MRSA菌株引起的感染也显示出类似的体内作用,其ED50值分别为0.72 mg/kg和0.87 mg/kg。然而,Tigecycline对由GISA菌株引起的感染的作用最大,其ED50值为1.9 mg/kg,比Daptomycin (ED50 = 6.1 mg/kg) 的作用高3倍多。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Petersen P J, Bradford P A, Weiss W J, et al. In vitro and in vivo activities of tigecycline (GAR-936), daptomycin, and comparative antimicrobial agents against glycopeptide-intermediate Staphylococcus aureus and other resistant gram-positive pathogens[J]. Antimicrobial agents and chemotherapy, 2002, 46(8): 2595-2601.

质量控制

化学结构

Tigecycline

相关生物数据

Tigecycline