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甲磺酸替加環(huán)素
- names：
Tigecycline mesylate
- CAS號(hào)：
1135871-27-0
MDL Number： - MF(分子式)： C30H43N5O11S MW(分子量)： 681.75
- EINECS: Reaxys Number:
- Pubchem ID:78358330 Brand:BIOFOUNT
甲磺酸替加環(huán)素(1135871-27-0,GAR-936 mesylate)是一種廣譜的甘氨酰環(huán)素抗生素。甲磺酸替加環(huán)素對(duì)于大腸桿菌（MG1655血壓）的平均抑制濃度（MIC）約為125 ng / mL。甲磺酸替加環(huán)素對(duì)于鮑曼不動(dòng)桿菌（A. baumannii）的MIC50 和MIC90 分別為1和2 mg / L。平均MIC：125 ng / mL（大腸桿菌），MIC50：1 mg / mL（鮑曼不動(dòng)桿菌），MIC90：2 mg / mL（鮑曼不動(dòng)桿菌）。
| 貨品編碼 | 規(guī)格 | 純度 | 價(jià)格 (￥) | 現(xiàn)價(jià)(￥) | 特價(jià)(￥) | 庫存描述 | 數(shù)量 | 總計(jì) (￥) |
|---|---|---|---|---|---|---|---|---|
| YZM000230-10mg | 10mg | >97% | ￥ 838.00 | ￥ 838.00 | 1-3天 | ￥ 0.00 |
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| 中文別名 | 甲磺酸替加環(huán)素(1135871-27-0);替加環(huán)素(甲磺酸鹽);GAR-936甲磺酸酯;HY-B0117B;CS-1878;替加環(huán)素甲磺酸酯; |
| 英文別名 | Tigecycline mesylate(1135871-27-0);Tigecycline mesylate;Tigecycline (mesylate);GAR-936 mesylate;HY-B0117B;CS-1878; |
| CAS號(hào) | 1135871-27-0 |
| 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 |
| 溶解度Solubility | |
| 性狀 | Solid |
| 儲(chǔ)藏條件 Storage conditions | -20°C干燥 |
甲磺酸替加環(huán)素(1135871-27-0,GAR-936 mesylate)實(shí)驗(yàn)注意事項(xiàng)：
1.實(shí)驗(yàn)前需戴好防護(hù)眼鏡，穿戴防護(hù)服和口罩，佩戴手套，避免與皮膚接觸。
2.實(shí)驗(yàn)過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時(shí)實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對(duì)實(shí)驗(yàn)人員造成傷害
3.實(shí)驗(yàn)后產(chǎn)生的廢棄物需分類存儲(chǔ)，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)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.
Tags:甲磺酸替加環(huán)素試劑,甲磺酸替加環(huán)素雜質(zhì),甲磺酸替加環(huán)素合成,甲磺酸替加環(huán)素中間體,甲磺酸替加環(huán)素密度,甲磺酸替加環(huán)素閃點(diǎn),甲磺酸替加環(huán)素溶解度,甲磺酸替加環(huán)素旋光度,甲磺酸替加環(huán)素蒸氣壓,甲磺酸替加環(huán)素購買,
| 產(chǎn)品說明 | 甲磺酸替加環(huán)素(1135871-27-0,GAR-936 mesylate)是一種有效的廣譜的甘氨酰環(huán)素抗生素 |
| Introduction | 甲磺酸替加環(huán)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 | 替加環(huán)素甲磺酸酯化是一種一流的，廣譜的抗生素，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 |
甲磺酸替加環(huán)素(1135871-27-0,GAR-936 mesylate)藥理學(xué)：
1甲磺酸替加環(huán)素是一種一流的，廣譜的抗生素，具有抗抗生素抗性生物的活性。
2、Tigecycline（0.63-30 µM，預(yù)孵育4天，處理72小時(shí)）用IC抑制AML2細(xì)胞和HL-60細(xì)胞50s為4.72±0.54和3.06±0.85μM（新鮮制備）。Tigecycline具有IC抑制AML2細(xì)胞和HL-60細(xì)胞的作用505.64±0.55和4.27±0.45μM（預(yù)孵育1天）的時(shí)間。Tigecycline具有IC抑制AML2細(xì)胞和HL-60細(xì)胞的作用505.02±0.60和4.39±0.44μM（預(yù)培養(yǎng)2天）的時(shí)間。Tigecycline具有IC抑制AML2細(xì)胞和HL-60細(xì)胞的作用50s為4.09±0.41和3.95±0.39μM（預(yù)培養(yǎng)3天）。在鹽水中預(yù)孵育Tigecycline 4天后，Tigecycline喪失了殺死TEX人白血病細(xì)胞的能力（來自IC50新鮮制備至IC時(shí)約為5 µM50預(yù)培養(yǎng)4天后> 50 µM），通過CellTiter Flour分析測定。
3、甲磺酸替加環(huán)素是一種一流的廣譜抗生素，對(duì)抗生素抗性生物具有活性。和社區(qū)獲得的細(xì)菌病原體。甲磺酸替加環(huán)素已顯示出通過與核糖體30S亞基結(jié)合并阻止氨基?；膖RNA容納在核糖體A位點(diǎn)來抑制翻譯延長步驟。甲磺酸替加環(huán)素也被發(fā)現(xiàn)可有效治療社區(qū)以及醫(yī)院獲得的呼吸機(jī)相關(guān)性肺炎和菌血癥，敗血癥伴休克和尿路感染。
1甲磺酸替加環(huán)素是一種一流的，廣譜的抗生素，具有抗抗生素抗性生物的活性。
2、Tigecycline（0.63-30 µM，預(yù)孵育4天，處理72小時(shí)）用IC抑制AML2細(xì)胞和HL-60細(xì)胞50s為4.72±0.54和3.06±0.85μM（新鮮制備）。Tigecycline具有IC抑制AML2細(xì)胞和HL-60細(xì)胞的作用505.64±0.55和4.27±0.45μM（預(yù)孵育1天）的時(shí)間。Tigecycline具有IC抑制AML2細(xì)胞和HL-60細(xì)胞的作用505.02±0.60和4.39±0.44μM（預(yù)培養(yǎng)2天）的時(shí)間。Tigecycline具有IC抑制AML2細(xì)胞和HL-60細(xì)胞的作用50s為4.09±0.41和3.95±0.39μM（預(yù)培養(yǎng)3天）。在鹽水中預(yù)孵育Tigecycline 4天后，Tigecycline喪失了殺死TEX人白血病細(xì)胞的能力（來自IC50新鮮制備至IC時(shí)約為5 µM50預(yù)培養(yǎng)4天后> 50 µM），通過CellTiter Flour分析測定。
3、甲磺酸替加環(huán)素是一種一流的廣譜抗生素，對(duì)抗生素抗性生物具有活性。和社區(qū)獲得的細(xì)菌病原體。甲磺酸替加環(huán)素已顯示出通過與核糖體30S亞基結(jié)合并阻止氨基?；膖RNA容納在核糖體A位點(diǎn)來抑制翻譯延長步驟。甲磺酸替加環(huán)素也被發(fā)現(xiàn)可有效治療社區(qū)以及醫(yī)院獲得的呼吸機(jī)相關(guān)性肺炎和菌血癥，敗血癥伴休克和尿路感染。
| 警示圖 | |
| 危險(xiǎn)性 | warning |
| 危險(xiǎn)性警示 | Not available |
| 安全聲明 | H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對(duì)身體有害 |
| 安全防護(hù) | P264處理后徹底清洗+P280戴防護(hù)手套/穿防護(hù)服/戴防護(hù)眼罩/戴防護(hù)面具+P305如果進(jìn)入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護(hù)理 |
| 備注 | 實(shí)驗(yàn)過程中防止吸入、食入，做好安全防護(hù) |
| 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. |
甲磺酸替加環(huán)素(1135871-27-0,GAR-936 mesylate)參考文獻(xiàn)：
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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