中文名 | Radezolid |
英文名 | Radezolid |
别名 | 雷德唑来 雷得唑来 雷得唑来RADEZOLID N-[[(5S)-3-[2-氟-4'-[[(1H-1,2,3-三唑-5-基甲基)氨基]甲基][1,1'-联苯]-4-基]-2-氧代-5-恶唑啉基]甲基]乙酰胺 |
英文别名 | RX1741 RX 1741 RX-1741 radezolid Radezolid Unii-53pc6lo35w N-[[(5S)-3-[2-Fluoro-4'-[[(1H-1,2,3-triazol-5-yLmethyl)amino]methyl][1,1'-biphenyl]-4-yl]-2-ox (5S)-N-[3-(2-fluoro-4'-{[(1H-[1,2,3]triazol-4-ylmethyl)amino]methyl}biphenyl-4-yl)-2-oxo-oxazolidin-5-ylmethyl]acetamide N-[[(5S)-3-[2-Fluoro-4'-[[(1H-1,2,3-triazol-5-ylmethyl)amino]methyl][1,1'-biphenyl]-4-yl]-2-oxo-5-oxazolidinyl]methyl]acetamide |
CAS | 869884-78-6 |
化学式 | C22H23FN6O3 |
分子量 | 438.45 |
密度 | 1.336 |
沸点 | 712.5±60.0 °C(Predicted) |
溶解度 | 溶于DMSO,不溶于水 |
酸度系数 | 15.53±0.46(Predicted) |
存储条件 | -20℃ |
体外研究 | Radezolid MICs are systematically equal to or lower (up to 3 log2 dilutions) than those of linezolid for all linezolid-susceptible strains, with an 8-fold difference for the linezolid-resistant strains. Radezolid shows a greater potency than linezolid, independent of the bacteria tested, when concentrations are expressed on a weight (mg/L) basis. Radezolid shows an improved potency compared to that of linezolid when concentrations are expressed on a weight (mg/L) basis. Radezolid and TR-700 perform well against 3-copy G2447T, G2576T, and G2576T/T2571C mutants. |
参考资料 展开查看 | 1: Bassetti M, Righi E. Safety profiles of old and new antimicrobials for the treatment of MRSA infections. Expert Opin Drug Saf. 2016 Jan 14. [Epub ahead of print] PubMed PMID: 26764972. 2: Kern WV. [New antibacterial agents on the market and in the pipeline]. Internist (Berl). 2015 Oct 18. [Epub ahead of print] German. PubMed PMID: 26475603. 3: Fulle S, Saini JS, Homeyer N, Gohlke H. Complex long-distance effects of mutations that confer linezolid resistance in the large ribosomal subunit. Nucleic Acids Res. 2015 Sep 18;43(16):7731-43. doi: 10.1093/nar/gkv729. Epub 2015 Jul 21. PubMed PMID: 26202966; PubMed Central PMCID: PMC4652758. 4: Mendes RE, Deshpande LM, Jones RN. Linezolid update: stable in vitro activity following more than a decade of clinical use and summary of associated resistance mechanisms. Drug Resist Updat. 2014 Apr;17(1-2):1-12. doi: 10.1016/j.drup.2014.04.002. Epub 2014 Apr 6. Review. PubMed PMID: 24880801. 5: Saini JS, Homeyer N, Fulle S, Gohlke H. Determinants of the species selectivity of oxazolidinone antibiotics targeting the large ribosomal subunit. Biol Chem. 2013 Nov;394(11):1529-41. doi: 10.1515/hsz-2013-0188. PubMed PMID: 24006327。 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.281 ml | 11.404 ml | 22.808 ml |
5 mM | 0.456 ml | 2.281 ml | 4.562 ml |
10 mM | 0.228 ml | 1.14 ml | 2.281 ml |
5 mM | 0.046 ml | 0.228 ml | 0.456 ml |
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