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Radezolid

现货
Catalog No.
A3749
新型的恶唑烷酮类抗生素
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,740.00
现货
5mg
¥ 1,660.00
现货
10mg
¥ 2,790.00
现货
50mg
¥ 6,350.00
现货

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Background

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

文献引用

1.Katarzyna Michalska, Elżbieta Bednarek, et al. "Comprehensive spectral identification of key intermediates to the final product of the chiral pool synthesis of radezolid." Chemistry Central Journal (2017) 11:82.
2.Michalska K, Gruba E, et al. "Application of spectroscopic methods (FT-IR, Raman, ECD and NMR) in studies of identification and optical purity of radezolid." Spectrochim Acta A Mol Biomol Spectrosc. 2017 Apr 20;183:116-122. PMID:28456082
3.Michalska K, Gruba E, et al. "Enantioselective recognition of radezolid by cyclodextrin modified capillary electrokinetic chromatography and electronic circular dichroism." J Pharm Biomed Anal. 2017 May 30;139:98-108. PMID:28279932

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt438.45
Cas No.869884-78-6
FormulaC22H23FN6O3
SynonymsRX-1741;RX 1741;RX1741
Solubility≥43.8 mg/mL in DMSO, ≥18.08 mg/mL in EtOH with gentle warming, <2.31 mg/mL in H2O
Chemical NameN-[[(5S)-3-[3-fluoro-4-[4-[(2H-triazol-4-ylmethylamino)methyl]phenyl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
SDFDownload SDF
Canonical SMILESCC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)C3=CC=C(C=C3)CNCC4=NNN=C4)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

Description Radezolid(INN,RX-1741)是一种新型的恶唑烷酮类抗生素。
靶点            
IC50            

质量控制

化学结构

Radezolid

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