Tedizolid HCl |
| رقم الكتالوجGC15288 |
Oxazolidinone for gram-positive infections
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: N/A
Sample solution is provided at 25 µL, 10mM.
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IC50: for MAO-A (monoamine oxidase-A), 8.7 uM; for MAO-B, 5.7 uM.
Tedizolid HCl is a reversible, novel oxazolidinone antibiotic. It is the first oxazolidinone to be approved since linezolid in 2000. Tedizolid phosphate is the second commercially available oxazolidinone antibiotic and is the prodrug form of tedizolid with a fixed once-daily dose. As an expanded-spectrum oxazolidinone it has potent activity against a wide range of Gram-positive pathogens [1].
In vitro: In vitro, tedizolid was a reversible inhibitor for both human MAO-A and MAO-B; for MAO-A, the value of IC50 was 8.7 uM, and for MAO-B, the value of IC50 was 5.7 uM. For this two inhibitions, add 46.0 and 2.1 uM of linezolid, respectively would be better [2].
In vivo: It exhibited not only a potent activity against Gram-positive pathogens but also maintained activity against linezolid resistant bacteria. In murine serotonergic model, the number of head twitches was analyzed after tedizolid phosphate was administrated by intraperitoneal injection [2].
Clinical trial: With 200 mg once daily tedizolid would treat the acute bacterial skin and skin structure infections caused by gram-positive bacteria in phase III clinical trials. The treatment effects of tedizolid for ventilator-acquired and health care-associated pneumonia were currently investigated [3].
References:
[1] Chen KH, Huang YT, Liao CH et dl. In Vitro Activities of Tedizolid and Linezolid against Gram-Positive Cocci Associated with Acute Bacterial Skin and Skin Structure Infections and Pneumonia. Antimicrob Agents Chemother. 2015 Oct;59(10):6262-5.
[2] S. Flanagan, K. Bartizal, S. L. Minassian et dl. In Vitro, In Vivo, and Clinical Studies of Tedizolid To Assess the Potential for Peripheral or Central Monoamine Oxidase Interactions. Antimicrob Agents Chemother. 2013 Jul;57(7):3060-6.
[3] Rybak JM, Marx K, Martin CA. Early experience with tedizolid: clinical efficacy, pharmacodynamics, and resistance. Pharmacotherapy. 2014 Nov;34(11):1198-208.
| Cas No. | N/A | SDF | |
| Chemical Name | (R)-3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one hydrochloride | ||
| Canonical SMILES | FC1=CC(N2C[C@H](CO)OC2=O)=CC=C1C3=CC=C(C4=NN(C)N=N4)N=C3.Cl | ||
| Formula | C17H16ClFN6O3 | M.Wt | 406.8 |
| الذوبان | ≥ 13.57mg/mL in DMSO with gentle warming, Limited solubility in EtOH | Storage | Store at -20°C |
| 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4582 mL | 12.2911 mL | 24.5821 mL |
| 5 mM | 0.4916 mL | 2.4582 mL | 4.9164 mL |
| 10 mM | 0.2458 mL | 1.2291 mL | 2.4582 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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 7 reference(s) in Google Scholar.)
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