Radezolid (Synonyms: Rx-01_667, RX-1741) |
Catalog No.GC13613
One-Click Copy Product Info
|
An oxazolidinone antibiotic
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 869884-78-6
Sample solution is provided at 25 µL, 10mM.
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Radezolid Description:
MIC90: Radezolid was approximately four-times more potent than linezolid against MRSA, with MIC90 of 0.5 mg/l and 2.0 mg/l, respectively [1].
Radezolid is an investigational oxazolidinone with excellent in vitro and in vivo activity against a variety of Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA). Effcacy has been attributed to the finding that radezolid accumulates in vitro in macrophages, polymorphonuclear leukocytes (PMNs), epithelial and endothelial cells.
In vitro: A study found that radezolid accumulated to similar levels (~10-fold) in all cell types (human keratinocytes, endothelial cells, bronchial epithelial cells, osteoblasts, macrophages, and rat embryo fibroblasts). At equivalent weight concentrations, radezolid proved consistently 10-fold more potent than linezolid in all these models, irrespective of the bacterial species and resistance phenotype or of the cell type infected. These data suggest the potential interest of radezolid for recurrent or persistent infections where intracellular foci play a determinant role [2].
In vivo: When administered at 50 mg/kg, radezolid and linezolid showed comparable reductions in bacterial burden 24 hours after inoculation. Area under the curve (AUC) analysis of tissue concentrations demonstrated that radezolid accumulated 2.4-fold in infected thighs when compared to non-infected thigh tissue (table). Linezolid showed no accumulation in infected thighs [3].
Clinical trial: Radezolid (INN, codenamed RX-1741) is developed by Rib-X Pharmaceuticals, Inc. for the treatment of serious multi-drug–resistant infections. Radezolid has completed two phase-II clinical trials. One of these clinical trials was for uncomplicated skin and skin-structure infections (uSSSI) and the other clinical trial was for community acquired pneumonia (CAP) (http://en.wikipedia.org/wiki/Radezolid)..
Reference:
[1] Laura Lawrence, Paul Danese, Joe DeVito, Francois Franceschi, and Joyce Sutcliffe. In Vitro Activities of the Rx-01 Oxazolidinones against Hospital and Community Pathogens. Antimicrob Agents Chemother. 2008; 52(5): 1653–1662.
[2] Lemaire S, Kosowska-Shick K, Appelbaum PC, Verween G, Tulkens PM, Van Bambeke F. Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila. Antimicrob Agents Chemother. 2010;54(6):2549-59.
[3] Burak E, Bortolon E, Molstad D, Jing H and Wu Y. Radezolid, a novel oxazolidinone, accumulates in infected thigh tissue. Post A1-1938. 49th ICAAC San Francisco, CA, USA September 12-15, 2009
Cell experiment: | Antibiotic accumulation is determined following the general procedure, and the cellular content of [14C]radezolid is assayed in cell lysates by liquid scintillation counting (lowest limit of detection, 0.003 mg/liter; linear response between 0.01 and 0.78 mg/liter; R2=0.999). All cell drug contents are expressed by reference to the total cell protein content and converted into apparent total cell concentrations using a conversion factor of 5 μL per mg of cell protein. |
References: [1]. Lemaire S, et al. Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila. | |
| Cas No. | 869884-78-6 | SDF | |
| Synonyms | Rx-01_667, RX-1741 | ||
| Chemical Name | N-[[(5S)-3-[3-fluoro-4-[4-[(2H-triazol-4-ylmethylamino)methyl]phenyl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide | ||
| Canonical SMILES | CC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)C3=CC=C(C=C3)CNCC4=NNN=C4)F | ||
| Formula | C22H23FN6O3 | M.Wt | 438.45 |
| Solubility | ≥ 43.8 mg/mL in DMSO, ≥ 18.08 mg/mL in EtOH with gentle warming | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2808 mL | 11.4038 mL | 22.8076 mL |
| 5 mM | 456.2 μL | 2.2808 mL | 4.5615 mL |
| 10 mM | 228.1 μL | 1.1404 mL | 2.2808 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)