| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
All bacteria that were susceptible to linezolid had radarzolid MICs that were either the same or lower than those of linezolid (up to 3 log2 dilutions); strains that were resistant to linezolid had an 8-fold difference in MICs. Regardless of the bacteria examined, Radezolid shown greater potency than Nezolid when concentrations were expressed on a weight basis (mg/L). In comparison to linezolid, radezolid is more potent when concentrations are expressed on a weight basis (mg/L) [1]. When it comes to 3-copy G2447T, G2576T, and G2576T/T2571C mutants, radezolid and TR-700 work effectively [2].
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| 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.
[2]. Locke JB, et al. Structure-activity relationships of diverse oxazolidinones for linezolid-resistant Staphylococcus aureus strains possessing the cfr methyltransferase gene or ribosomal mutations. Antimicrob Agents Chemother. 2010 Dec;54(12):5337-43 |
| Additional Infomation |
Radezolid has been used in trials studying the treatment of Abscess, Bacterial Skin Diseases, Streptococcal Infections, Infectious Skin Diseases, and Staphylococcal Skin Infections, among others.
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| Molecular Formula |
C22H23FN6O3
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|---|---|
| Molecular Weight |
438.4634
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| Exact Mass |
438.181
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| CAS # |
869884-78-6
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| Related CAS # |
869884-78-6;869884-77-5 (HCl);
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| PubChem CID |
11224409
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
712.5±60.0 °C at 760 mmHg
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| Flash Point |
384.7±32.9 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.612
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| LogP |
2.28
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
647
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C1O[C@@H](CNC(=O)C)CN1C1C=CC(C2C=CC(CNCC3NN=NC=3)=CC=2)=C(F)C=1
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| InChi Key |
BTTNOGHPGJANSW-IBGZPJMESA-N
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| InChi Code |
InChI=1S/C22H23FN6O3/c1-14(30)25-12-19-13-29(22(31)32-19)18-6-7-20(21(23)8-18)16-4-2-15(3-5-16)9-24-10-17-11-26-28-27-17/h2-8,11,19,24H,9-10,12-13H2,1H3,(H,25,30)(H,26,27,28)/t19-/m0/s1
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| 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
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| Synonyms |
RX-1741 RX1741 RX 1741 Radezolid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 25 mg/mL (~57.02 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2807 mL | 11.4035 mL | 22.8071 mL | |
| 5 mM | 0.4561 mL | 2.2807 mL | 4.5614 mL | |
| 10 mM | 0.2281 mL | 1.1404 mL | 2.2807 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00640926 | COMPLETEDWITH RESULTS | Drug: Radezolid Drug: Radezolid Drug: Radezolid |
Community-Acquired Pneumonia (CAP) | Melinta Therapeutics, Inc. | 2007-10 | Phase 2 |
| NCT00646958 | COMPLETEDWITH RESULTS | Drug: Radezolid Drug: Radezolid Drug: Linezolid |
Abscess Bacterial Skin Diseases Infectious Skin Diseases Staphylococcal Skin Infections Streptococcal Infections |
Melinta Therapeutics, Inc. | 2007-12 | Phase 2 |
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