Radezolid
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
MIC90:Radezolid对耐甲氧西林金黄色葡萄球菌(MRSA)的作用比Linezolid高约4倍,相应MIC90为0.5 mg/l和2.0 mg/l[1]。
Radezolid是一种实验用恶唑烷酮,具有优异的体内外活性,有效对抗各种革兰氏阳性菌,包括MRSA。体外实验表明,Radezolid可以积聚于巨噬细胞、多形核白细胞(PMNs),上皮细胞和内皮细胞,从而发挥其抗菌作用。
体外:一项研究发现,Radezolid在所有类型的细胞(人角质形成细胞、内皮细胞、支气管上皮细胞、成骨细胞、巨噬细胞以及大鼠胚胎成纤维细胞)中具有相似的积累量(~10倍)。在所有这些模型中,不论细菌种类、耐药表型或感染的细胞类型,在相等质量浓度下,Radezolid的抗菌作用均比Linezolid高10倍。上述数据表明,Radezolid的胞内积累量在治疗细胞复发性或持续性感染中起着决定性作用[2]。
体内:接种24小时后,50 mg/kg的Radezolid和Linezolid表现出相当的细菌负荷减少。组织药物浓度的曲线下面积(AUC)分析表明,相对于未受感染的大腿组织,Radezolid在受感染大腿中的积累量为2.4倍。Linezolid没有积聚于受感染的大腿[3]。
临床试验:Radezolid(INN,RX-1741)由Rib-X制药有限公司研发,用于治疗严重的多重耐药菌感染。Radezolid已完成了两项II期临床试验。上述两项临床试验分别验证了Radezolid对无并发症皮肤及皮肤结构感染(uSSSI)和社区获得性肺炎(CAP)的疗效(http://en.wikipedia.org/wiki/Radezolid)。
参考文献:
[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.
- 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
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 438.45 |
Cas No. | 869884-78-6 |
Formula | C22H23FN6O3 |
Synonyms | RX-1741;RX 1741;RX1741 |
Solubility | ≥43.8 mg/mL in DMSO; insoluble in H2O; ≥18.08 mg/mL in EtOH with gentle warming |
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 |
SDF | Download SDF |
Canonical SMILES | CC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)C3=CC=C(C=C3)CNCC4=NNN=C4)F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
人类THP-1细胞 |
溶解方法 |
在DMSO中的溶解度 ≥43.8mg / mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
1mg/l,4mg/l,20mg/l |
应用 |
Radezolid在肉汤和人类THP-1细胞两种环境中对金黄色葡萄球菌的抑制作用表现出时间依赖性。当浓度低至1 mg / L时,Radezolid导致细胞外环境中金黄色葡萄球菌2 log10 CFU降低,细胞内0.5至1 log10 CFU降低。 |
References: [1]. 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 Jun;54(6):2549-59. doi: 10.1128/AAC.01724-09.Epub 2010 Apr 12. PubMed PMID: 20385852; PubMed Central PMCID: PMC2876393. |
Description | Radezolid(INN,RX-1741)是一种新型的恶唑烷酮类抗生素。 | |||||
靶点 | ||||||
IC50 |
质量控制和MSDS
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