Omadacycline tosylate
(Synonyms: 奥马环素; PTK 0796 tosylate; Amadacycline tosylate) 目录号 : GC36805
Omadacycline tosylate是一种新型氨基甲基环素类抗生素。
Cas No.:1075240-43-5
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
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Animal experiment [1]: |
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Animal models |
Female ICR/Swiss mice |
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Preparation method |
Mice were rendered neutropenic (neutrophils < 100/mm3) by injecting cyclophosphamide intraperitoneally before lung infection. Lung infections with each of the S. pneumoniae strains were produced by the administration of 50 μl of inoculum into the nares of isoflurane-anesthetized mice. Therapy with omadacycline tosylate initiated 2 h after induction of infection. |
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Dosage form |
0.5、2、8、32mg/kg; i.d |
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Applications |
Omacycline tosylate has bactericidal activity at experimental doses. |
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References: [1]. Lepak AJ, Zhao M,et,al. In Vivo Pharmacodynamic Evaluation of Omadacycline (PTK 0796) against Streptococcus pneumoniae in the Murine Pneumonia Model. Antimicrob Agents Chemother. 2017 Apr 24;61(5):e02368-16. doi: 10.1128/AAC.02368-16. PMID: 28193651; PMCID: PMC5404567. |
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Omadacycline tosylate is a newly developed aminomethylcycline antibiotic with applications in acute bacterial skin and skin structure infections (ABSSSI) as well as community-acquired bacterial pneumonia (CABP). Derived from minocycline, omadacycline shares similar mechanisms of action with other tetracyclines, inhibiting bacterial protein synthesis by binding to the 30S ribosomal subunit. Notably, omadacycline exhibits broad-spectrum antibacterial properties effective against a range of Gram-positive and Gram-negative aerobic, anaerobic, and atypical bacteria[1-4].
Omadacycline tosylate (0.5、2、8、32mg/kg; i.d) has shown strong efficacy in vivo against specific strains of Streptococcus pneumoniae, with bactericidal activity at all experimental doses [5]. Omacycline tosylate (0.25–64 mg/kg) has potent activity against Staphylococcus aureus, including methicillin-susceptible S. aureus (MSSA) and methicillin-resistant S. aureus (MRSA) in the neutropenic murine thigh infection model [6]. Mice treated with 15 mg/kg is efficacious in a murine model of pulmonary infection due to M. abscessus. Reduction in the CFU counts of Mycobacteroides abscessus Clinical Isolates in the lungs of mice occurred after 2 weeks of treatment with omadacycline tosylate [7]
References:
[1]. Zhanel GG, Esquivel J, et,al. Omadacycline: A Novel Oral and Intravenous Aminomethylcycline Antibiotic Agent. Drugs. 2020 Feb;80(3):285-313. doi: 10.1007/s40265-020-01257-4. PMID: 31970713.
[2]. Gallagher JC. Omadacycline: A Modernized Tetracycline. Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S1-S5. doi: 10.1093/cid/ciz394. PMID: 31367739; PMCID: PMC6669280.
[3]. Watkins RR, Deresinski S. Omadacycline: A Novel Tetracycline Derivative With Oral and Intravenous Formulations. Clin Infect Dis. 2019 Aug 16;69(5):890-896. doi: 10.1093/cid/ciz242. PMID: 30893428.
[4]. Karlowsky JA, Steenbergen J, et,al. Microbiology and Preclinical Review of Omadacycline. Clin Infect Dis. 2019 Aug 1;69(Suppl 1):S6-S15. doi: 10.1093/cid/ciz395. PMID: 31367743; PMCID: PMC6669291.
[5]. Lepak AJ, Zhao M, et,al. In Vivo Pharmacodynamic Evaluation of Omadacycline (PTK 0796) against Streptococcus pneumoniae in the Murine Pneumonia Model. Antimicrob Agents Chemother. 2017 Apr 24;61(5):e02368-16. doi: 10.1128/AAC.02368-16. PMID: 28193651; PMCID: PMC5404567.
[6]. Lepak AJ, Zhao M, et,al. In Vivo Pharmacodynamics of Omadacycline against Staphylococcus aureus in the Neutropenic Murine Thigh Infection Model. Antimicrob Agents Chemother. 2019 Jun 24;63(7):e00624-19. doi: 10.1128/AAC.00624-19. PMID: 31036691; PMCID: PMC6591633.
[7]. Nicklas DA, Maggioncalda EC, et,al. Potency of Omadacycline against Mycobacteroides abscessus Clinical Isolates In Vitro and in a Mouse Model of Pulmonary Infection. Antimicrob Agents Chemother. 2022 Jan 18;66(1):e0170421. doi: 10.1128/AAC.01704-21. Epub 2021 Oct 18. PMID: 34662184; PMCID: PMC8765394.
Omadacycline tosylate是一种新型氨基甲基环素类抗生素。可用于急性细菌性皮肤及皮肤结构感染(ABSSSI)和社区获得性细菌性肺炎(CABP)。Omadacycline是米诺环素的衍生物。与其他四环素类似，Omadacycline tosylate通过结合30S核糖体亚基抑制细菌蛋白质合成。Omadacycline tosylate对革兰氏阳性和革兰氏阴性好氧、厌氧和非典型细菌具有广谱抗菌活性[1-4]。
Omadacycline tosylate (0.5、2、8、32mg/kg; i.d)在体内对特定的肺炎链球菌菌株显示出很强的疗效，在所有实验剂量下都具有杀菌活性[5]。在中性粒细胞减少小鼠大腿感染模型中，Omadacycline tosylate (0.25–64 mg/kg)对包括甲氧西林敏感金黄色葡萄球菌(MSSA)和耐甲氧西林金黄色葡萄球菌(MRSA)在内的金黄色葡萄球菌具有强效活性[6]。Omadacycline tosylate在15 mg/kg剂量对小鼠脓肿支原体肺部感染模型有效，用Omadacycline tosylate治疗2周后，小鼠肺部脓肿分枝杆菌临床分离株CFU计数减少[7]。
| Cas No. | 1075240-43-5 | SDF | |
| 别名 | 奥马环素; PTK 0796 tosylate; Amadacycline tosylate | ||
| Canonical SMILES | CC1=CC=C(S(=O)(O)=O)C=C1.O=C(C2=C(O)[C@@H](N(C)C)[C@@](C[C@@]3([H])C(C(C4=C(O)C(CNCC(C)(C)C)=CC(N(C)C)=C4C3)=O)=C5O)([H])[C@@]5(O)C2=O)N | ||
| 分子式 | C36H48N4O10S | 分子量 | 728.85 |
| 溶解度 | DMSO : 100mg/mL; Water : 100mg/mL | 储存条件 | 4°C, protect from light |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.372 mL | 6.8601 mL | 13.7202 mL |
| 5 mM | 0.2744 mL | 1.372 mL | 2.744 mL |
| 10 mM | 0.1372 mL | 0.686 mL | 1.372 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。