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甲磺酸替加环素
- names：
Tigecycline mesylate
- CAS号：
1135871-27-0
MDL Number： - MF(分子式)： C30H43N5O11S MW(分子量)： 681.75
- EINECS: Reaxys Number:
- Pubchem ID:78358330 Brand:BIOFOUNT
甲磺酸替加环素(1135871-27-0,GAR-936 mesylate)是一种广谱的甘氨酰环素抗生素。甲磺酸替加环素对于大肠杆菌（MG1655血压）的平均抑制浓度（MIC）约为125 ng / mL。甲磺酸替加环素对于鲍曼不动杆菌（A. baumannii）的MIC50 和MIC90 分别为1和2 mg / L。平均MIC：125 ng / mL（大肠杆菌），MIC50：1 mg / mL（鲍曼不动杆菌），MIC90：2 mg / mL（鲍曼不动杆菌）。
| 货品编码 | 规格 | 纯度 | 价格 (¥) | 现价(¥) | 特价(¥) | 库存描述 | 数量 | 总计 (¥) |
|---|---|---|---|---|---|---|---|---|
| YZM000230-10mg | 10mg | >97% | ¥ 838.00 | ¥ 838.00 | 1-3天 | ¥ 0.00 |
| 中文别名 | 甲磺酸替加环素(1135871-27-0);替加环素(甲磺酸盐);GAR-936甲磺酸酯;HY-B0117B;CS-1878;替加环素甲磺酸酯; |
| 英文别名 | Tigecycline mesylate(1135871-27-0);Tigecycline mesylate;Tigecycline (mesylate);GAR-936 mesylate;HY-B0117B;CS-1878; |
| CAS号 | 1135871-27-0 |
| SMILES | O=C(C(C1=O)=C(O)[C@@H](N(C)C)[C@]2([H])C[C@]3([H])CC4=C(C(C3=C(O)[C@@]21O)=O)C(O)=C(NC(CNC(C)(C)C)=O)C=C4N(C)C)N.O=S(C)(O)=O |
| Inchi | InChI=1S/C29H39N5O8.CH4O3S/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;1-5(2,3)4/h10,12,14,21,31,36,38-39,42H,8-9,11H2,1-7H3,(H2,30,41)(H,32,35);1H3,(H,2,3,4)/t12-,14-,21-,29-;/m0./s1 |
| InchiKey | JYPFQXOJRDSKSF-KXLOKULZSA-N |
| 分子式 Formula | C30H43N5O11S |
| 分子量 Molecular Weight | 681.75 |
| 闪点 FP | |
| 熔点 Melting point | No data available |
| 沸点 Boiling point | |
| Polarizability极化度 | |
| 密度 Density | |
| 蒸汽压 Vapor Pressure | |
| 溶解度Solubility | |
| 性状 | Solid |
| 储藏条件 Storage conditions | -20°C干燥 |
甲磺酸替加环素(1135871-27-0,GAR-936 mesylate)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
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| 产品说明 | 甲磺酸替加环素(1135871-27-0,GAR-936 mesylate)是一种有效的广谱的甘氨酰环素抗生素 |
| Introduction | 甲磺酸替加环素(1135871-27-0,GAR-936 mesylate)is a broadpectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline forE. coli(MG1655 strain) is approximately 125 ng/mL. |
| Application1 | 替加环素甲磺酸酯化是一种一流的，广谱的抗生素，具有抗抗生素抗性生物的活性。 |
| Application2 | MIC50and MIC90are 1 and 2 mg/L forAcinetobacter baumannii(A. baumannii), respectively. |
| Application3 |
甲磺酸替加环素(1135871-27-0,GAR-936 mesylate)药理学：
1甲磺酸替加环素是一种一流的，广谱的抗生素，具有抗抗生素抗性生物的活性。
2、Tigecycline（0.63-30 µM，预孵育4天，处理72小时）用IC抑制AML2细胞和HL-60细胞50s为4.72±0.54和3.06±0.85μM（新鲜制备）。Tigecycline具有IC抑制AML2细胞和HL-60细胞的作用505.64±0.55和4.27±0.45μM（预孵育1天）的时间。Tigecycline具有IC抑制AML2细胞和HL-60细胞的作用505.02±0.60和4.39±0.44μM（预培养2天）的时间。Tigecycline具有IC抑制AML2细胞和HL-60细胞的作用50s为4.09±0.41和3.95±0.39μM（预培养3天）。在盐水中预孵育Tigecycline 4天后，Tigecycline丧失了杀死TEX人白血病细胞的能力（来自IC50新鲜制备至IC时约为5 µM50预培养4天后> 50 µM），通过CellTiter Flour分析测定。
3、甲磺酸替加环素是一种一流的广谱抗生素，对抗生素抗性生物具有活性。和社区获得的细菌病原体。甲磺酸替加环素已显示出通过与核糖体30S亚基结合并阻止氨基酰化的tRNA容纳在核糖体A位点来抑制翻译延长步骤。甲磺酸替加环素也被发现可有效治疗社区以及医院获得的呼吸机相关性肺炎和菌血症，败血症伴休克和尿路感染。
1甲磺酸替加环素是一种一流的，广谱的抗生素，具有抗抗生素抗性生物的活性。
2、Tigecycline（0.63-30 µM，预孵育4天，处理72小时）用IC抑制AML2细胞和HL-60细胞50s为4.72±0.54和3.06±0.85μM（新鲜制备）。Tigecycline具有IC抑制AML2细胞和HL-60细胞的作用505.64±0.55和4.27±0.45μM（预孵育1天）的时间。Tigecycline具有IC抑制AML2细胞和HL-60细胞的作用505.02±0.60和4.39±0.44μM（预培养2天）的时间。Tigecycline具有IC抑制AML2细胞和HL-60细胞的作用50s为4.09±0.41和3.95±0.39μM（预培养3天）。在盐水中预孵育Tigecycline 4天后，Tigecycline丧失了杀死TEX人白血病细胞的能力（来自IC50新鲜制备至IC时约为5 µM50预培养4天后> 50 µM），通过CellTiter Flour分析测定。
3、甲磺酸替加环素是一种一流的广谱抗生素，对抗生素抗性生物具有活性。和社区获得的细菌病原体。甲磺酸替加环素已显示出通过与核糖体30S亚基结合并阻止氨基酰化的tRNA容纳在核糖体A位点来抑制翻译延长步骤。甲磺酸替加环素也被发现可有效治疗社区以及医院获得的呼吸机相关性肺炎和菌血症，败血症伴休克和尿路感染。
| 警示图 | |
| 危险性 | warning |
| 危险性警示 | Not available |
| 安全声明 | H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害 |
| 安全防护 | P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理 |
| 备注 | 实验过程中防止吸入、食入，做好安全防护 |
| Jitkova Y, et al. A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity. PLoS One. 2014 May 28;9(5):e95281. |
| Falagas ME, et al. Activity of TP-6076 against carbapenem-resistant Acinetobacter baumannii isolates collected from inpatients in Greek hospitals. Int J Antimicrob Agents. 2018 Aug;52(2):269-271. |
甲磺酸替加环素(1135871-27-0,GAR-936 mesylate)参考文献：
1、Activity of TP-6076 against carbapenem-resistant Acinetobacter baumannii isolates collected from inpatients in Greek hospitals
Matthew E Falagas 1, Tilemachos Skalidis 2, Konstantinos Z Vardakas 3, Georgios L Voulgaris 4, Georgios Papanikolaou 5, Nicholas Legakis 2, Hellenic TP-6076 Study Group
Abstract TP-6076 is a synthetic fluorocycline antibiotic that inhibits bacterial protein synthesis. In this study, carbapenem-resistant Acinetobacter baumannii clinical isolates from 13 Greek hospitals were tested for susceptibility to TP-6076 and comparator antibiotics. Broth microdilution plates were used to determine minimum inhibitory concentrations (MICs). A total of 121 non-duplicate A. baumannii isolates were tested. The MIC50 and MIC90 values of TP-6076 were 0.03 mg/L and 0.06 mg/L, respectively. Tigecycline was the second most active antibiotic (MIC90, 2 mg/L), followed by minocycline (MIC90, 8 mg/L). TP-6076 exhibited MIC90 values that were one dilution lower against tigecycline- and minocycline-susceptible isolates than against resistant isolates. There was no difference in the MIC90 value for colistin-susceptible or -resistant isolates. In conclusion, TP-6076 exhibited greater antimicrobial activity in vitro against carbapenem-resistant A. baumannii than comparator antibiotics.
2、A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity
Yulia Jitkova 1, Marcela Gronda 1, Rose Hurren 1, Xiaoming Wang 1, Carolyn A Goard 1, Bozhena Jhas 1, Aaron D Schimmer
Abstract Tigecycline is a broad-spectrum, first-in-class glycylcycline antibiotic currently used to treat complicated skin and intra-abdominal infections, as well as community-acquired pneumonia. In addition, we have demonstrated that tigecycline also has in vitro and in vivo activity against acute myeloid leukemia (AML) due to its ability to inhibit mitochondrial translation. Tigecycline is relatively unstable after reconstitution, and this instability may limit the use of the drug in ambulatory infusions for the treatment of infection and may prevent the development of optimal dosing schedules for the treatment of AML. This study sought to identify a formulation that improved the stability of the drug after reconstitution and maintained its antimicrobial and antileukemic activity. A panel of chemical additives was tested to identify excipients that enhanced the stability of tigecycline in solution at room temperature for up to one week. We identified a novel formulation containing the oxygen-reducing agents ascorbic acid (3 mg/mL) and pyruvate (60 mg/mL), in saline solution, pH 7.0, in which tigecycline (1 mg/mL) remained intact when protected from light for at least 7 days. This formulation also preserved the drug's antibacterial and antileukemic activity in vitro. Moreover, the novel formulation retained tigecycline's antileukemic activity in vivo. Thus, we identified and characterized a novel formulation for tigecycline that preserves its stability and efficacy after reconstitution.
1、Activity of TP-6076 against carbapenem-resistant Acinetobacter baumannii isolates collected from inpatients in Greek hospitals
Matthew E Falagas 1, Tilemachos Skalidis 2, Konstantinos Z Vardakas 3, Georgios L Voulgaris 4, Georgios Papanikolaou 5, Nicholas Legakis 2, Hellenic TP-6076 Study Group
Abstract TP-6076 is a synthetic fluorocycline antibiotic that inhibits bacterial protein synthesis. In this study, carbapenem-resistant Acinetobacter baumannii clinical isolates from 13 Greek hospitals were tested for susceptibility to TP-6076 and comparator antibiotics. Broth microdilution plates were used to determine minimum inhibitory concentrations (MICs). A total of 121 non-duplicate A. baumannii isolates were tested. The MIC50 and MIC90 values of TP-6076 were 0.03 mg/L and 0.06 mg/L, respectively. Tigecycline was the second most active antibiotic (MIC90, 2 mg/L), followed by minocycline (MIC90, 8 mg/L). TP-6076 exhibited MIC90 values that were one dilution lower against tigecycline- and minocycline-susceptible isolates than against resistant isolates. There was no difference in the MIC90 value for colistin-susceptible or -resistant isolates. In conclusion, TP-6076 exhibited greater antimicrobial activity in vitro against carbapenem-resistant A. baumannii than comparator antibiotics.
2、A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity
Yulia Jitkova 1, Marcela Gronda 1, Rose Hurren 1, Xiaoming Wang 1, Carolyn A Goard 1, Bozhena Jhas 1, Aaron D Schimmer
Abstract Tigecycline is a broad-spectrum, first-in-class glycylcycline antibiotic currently used to treat complicated skin and intra-abdominal infections, as well as community-acquired pneumonia. In addition, we have demonstrated that tigecycline also has in vitro and in vivo activity against acute myeloid leukemia (AML) due to its ability to inhibit mitochondrial translation. Tigecycline is relatively unstable after reconstitution, and this instability may limit the use of the drug in ambulatory infusions for the treatment of infection and may prevent the development of optimal dosing schedules for the treatment of AML. This study sought to identify a formulation that improved the stability of the drug after reconstitution and maintained its antimicrobial and antileukemic activity. A panel of chemical additives was tested to identify excipients that enhanced the stability of tigecycline in solution at room temperature for up to one week. We identified a novel formulation containing the oxygen-reducing agents ascorbic acid (3 mg/mL) and pyruvate (60 mg/mL), in saline solution, pH 7.0, in which tigecycline (1 mg/mL) remained intact when protected from light for at least 7 days. This formulation also preserved the drug's antibacterial and antileukemic activity in vitro. Moreover, the novel formulation retained tigecycline's antileukemic activity in vivo. Thus, we identified and characterized a novel formulation for tigecycline that preserves its stability and efficacy after reconstitution.
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