Omadacycline tosylate |
| رقم الكتالوجGC36805 |
Omadacycline (PTK 0796) tosylate ، مضاد جرثومي أمينوميثيل سيكلين الأول من نوعه في فئته ، هو عضو في فئة التتراسيكلين من المضادات الحيوية
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1075240-43-5
Sample solution is provided at 25 µL, 10mM.
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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.
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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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| Cas No. | 1075240-43-5 | SDF | |
| 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 | ||
| Formula | C36H48N4O10S | M.Wt | 728.85 |
| الذوبان | DMSO : 100mg/mL; Water : 100mg/mL | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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