Eravacycline dihydrochloride (TP-434 dihydrochloride)
(Synonyms: 盐酸依拉环素,TP-434 dihydrochloride; TP-434-046) 目录号 : GC32061
Eravacycline (TP-434)是一种新型四环素(TET)抗生素。
Cas No.:1334714-66-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Bactericidal experiment[1]: | |
Bacterial strain | Escherichia coli isolate, EC200( uropathogenic, tetracycline-resistant, β-lactamase-producing) |
Preparation Method | Tubes with 24-hour pre-formed biofilms had their planktonic cells aseptically removed, after which medium containing the drug was added, and the tubes were incubated for another 24 hours. |
Reaction Conditions | 0.03 to 4 μg/ml; 24h |
Applications | Biofilms treated with Eravacycline dihydrochloride (TP-434 dihydrochloride)at concentrations of 0.25 μg/ml or higher exhibited decreased crystal violet staining. |
| Animal experiment [2]: | |
Animal models | BALB/c mice(Mouse lung infection model) |
Preparation Method | Mice were administered 50 μl of the prepared bacterial inoculum (tetracycline-resistant S. pneumoniae and MRSA isolates). TP-434, formulated in sterile 0.9% saline, was given to the mice through tail vein intravenous injection at 2 and 12 hours post-infection. |
Dosage form | 3-12mg/kg; i.v. |
Applications | Eravacycline dihydrochloride (TP-434 dihydrochloride)exhibits a clear therapeutic effect in mice infected with tetracycline-resistant S. pneumoniae and MRSA isolates. |
References: | |
Eravacycline dihydrochloride (TP-434 dihydrochloride)is a novel tetracycline (TET) antibiotic. It exhibits in vitro activity against various gram-positive, gram-negative aerobic and anaerobic pathogens, including those exhibiting TET-specific acquired resistance mechanisms[1]. It inhibits protein synthesis through binding to the 30S ribosomal subunit[2]. Eravacycline dihydrochloride (TP-434 dihydrochloride)was approved for the treatment of complicated intraabdominal infections (cIAIs) in adults[3-4].
Eravacycline dihydrochloride (TP-434 dihydrochloride)(0.03 to 4 μg/ml; 24h) showed obvious bacteriostatic effect on pre-established biofilms formed by a uropathogenic Escherichia coli strain in vitro[5]. Eravacycline (0-8 μg/ml) has antibacterial activity against a large panel of clinical M. abscessus isolates in vitro[6].
Eravacycline (3-12mg/kg) was injected intravenically through the tail vein 2 and 12 h after infection with tetracycline resistant Streptococcus pneumoniae and MRSA isolates. Eravacycline has obvious therapeutic effect on infected mice, for lung infections with MRSA SA191, eravacycline given at 10 mg/kg i.v. produced a 2.4 log10 CFU reduction versus the values for the 24-hour untreated controls.[7].
References:
[1]. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Eravacycline. 2019 Apr 10. PMID: 31643186.
[2]. Chopra I, Roberts M. Tetracycline antibiotics: mode of action, applications, molecular biology, and epidemiology of bacterial resistance. Microbiol Mol Biol Rev. 2001 Jun;65(2):232-60 ; second page, table of contents. doi: 10.1128/MMBR.65.2.232-260.2001. PMID: 11381101; PMCID: PMC99026.
[3]. Alosaimy S, Abdul-Mutakabbir JC, et,al. Evaluation of Eravacycline: A Novel Fluorocycline. Pharmacotherapy. 2020 Mar;40(3):221-238. doi: 10.1002/phar.2366. Epub 2020 Feb 21. PMID: 31944332.
[4]. Sutcliffe JA, O'Brien W, et,al. Antibacterial activity of eravacycline (TP-434), a novel fluorocycline, against hospital and community pathogens. Antimicrob Agents Chemother. 2013 Nov;57(11):5548-58. doi: 10.1128/AAC.01288-13. Epub 2013 Aug 26. PMID: 23979750; PMCID: PMC3811277.[5]. Grossman TH, O'Brien W, et,al. Eravacycline dihydrochloride (TP-434 dihydrochloride)is active in vitro against biofilms formed by uropathogenic Escherichia coli. Antimicrob Agents Chemother. 2015 Apr;59(4):2446-9. doi: 10.1128/AAC.04967-14. Epub 2015 Jan 26. PMID: 25624334; PMCID: PMC4356792.
[6]. Li A, He S, et,al. Omadacycline, Eravacycline, and Tigecycline Express Anti-Mycobacterium abscessus Activity In Vitro. Microbiol Spectr. 2023 Jun 15;11(3):e0071823. doi: 10.1128/spectrum.00718-23. Epub 2023 May 4. PMID: 37140428; PMCID: PMC10269442.
[7]. Grossman TH, Murphy TM, et,al. Eravacycline dihydrochloride (TP-434 dihydrochloride)is efficacious in animal models of infection. Antimicrob Agents Chemother. 2015 May;59(5):2567-71. doi: 10.1128/AAC.04354-14. Epub 2015 Feb 17. PMID: 25691636; PMCID: PMC4394802.
Eravacycline (TP-434)是一种新型四环素(TET)抗生素。TP-434在体外对各种革兰氏阳性、革兰氏阴性的好氧和厌氧病原体具有活性，包括那些表现出TET特异性获得性耐药机制的病原体[1]。Eravacycline通过与30S核糖体亚基结合抑制蛋白质合成[2]。Eravacycline可用于治疗成人并发腹腔内感染(cIAIs)[3-4]。
Eravacycline dihydrochloride (TP-434 dihydrochloride)(0.03 to 4 μg/ml; 24h)对尿路致病性大肠杆菌菌株形成的生物膜有明显的抑菌作用[5]。Eravacycline (0-8 μg/ml)在体外对临床脓肿分枝杆菌分离株具有抗菌活性[6]。
Eravacycline dihydrochloride (TP-434 dihydrochloride)(3-12mg/kg)在感染四环素耐药肺炎链球菌和MRSA分离株后2和12 h经尾静脉注射小鼠后对感染小鼠有明显的治疗作用, 对于MRSA SA191肺部感染，与未治疗组相比，10mg /kg静脉滴注Eravacycline可使CFU降低2.4 log10[7]。
| Cas No. | 1334714-66-7 | SDF | |
| 别名 | 盐酸依拉环素,TP-434 dihydrochloride; TP-434-046 | ||
| Canonical SMILES | O=C(NC(C(O)=C1C2=O)=CC(F)=C1C[C@@]3([H])C[C@@]4([H])[C@H](N(C)C)C(O)=C(C(N)=O)C([C@@]4(O)C(O)=C32)=O)CN5CCCC5.[H]Cl.[H]Cl | ||
| 分子式 | C27H33Cl2FN4O8 | 分子量 | 631.48 |
| 溶解度 | Water : 50 mg/mL (79.18 mM) | 储存条件 | -80°C, protect from light, stored under nitrogen,unstable in solution, ready to use. |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5836 mL | 7.9179 mL | 15.8358 mL |
| 5 mM | 0.3167 mL | 1.5836 mL | 3.1672 mL |
| 10 mM | 0.1584 mL | 0.7918 mL | 1.5836 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
A Novel Design Eco-friendly Microwave-assisted Cu-N@CQDs Sensor for the Quantification of Eravacycline via Spectrofluorimetric Method; Application to Greenness Assessments, Dosage Form and Biological Samples
J Fluoresc 2023 Mar 3.PMID:36867288DOI:10.1007/s10895-023-03190-7.
Community-acquired pneumonia is one of the most common infectious diseases and a substantial cause of mortality and morbidity worldwide. Therefore Eravacycline (ERV) was approved by the FDA in 2018 for the treatment of acute bacterial skin infections, GIT infections, and community-acquired bacterial pneumonia caused by susceptible bacteria. Hence, a green highly sensitive, cost-effective, fast, and selective fluorimetric approach was developed for the estimation of ERV in milk, dosage form, content uniformity, and human plasma. The selective method is based on the utilization of plum juice and copper sulphate for the synthesis of green copper and nitrogen carbon dots (Cu-N@CDs) with high quantum yield. The quantum dots' fluorescence was enhanced after the addition of ERV. The calibration range was found to be in the range 1.0 - 80.0 ng mL-1 with LOQ equal to 0.14 ng mL-1 and LOD was found to be 0.05 ng mL-1. The creative method is simple to deploy in clinical labs and therapeutic drug health monitoring system. The current approach has been bioanalytically validated using US-FDA and validated ICH criteria. High-resolution transmission electron microscopy (HR-TEM), X-ray photon spectroscopy (XPS), Zeta potential measurements, fluorescence, UV-VIS, and FTIR spectroscopy have all been used to fully characterize the Cu-N@CQDs. The Cu-N@CQDs were effectively applied in human plasma and milk samples with a high percentage of recovery ranging from 97.00 to 98.80%.