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.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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]。
| 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: | |
| 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。 |
||
| 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet