|(2S,3S,4R,6S)-6-(((2R,3S,4R,5R,6S)-6-(((4R,5S,6S,7R,9R,10R,11E,13E,16R)-4-乙酰氧基-10-羟基-5-甲氧基-9,16-二甲基-2-氧代-7-(2-氧代乙基)氧杂环十六烷基-11,13-二烯-6-基)氧基)-4-(二甲基氨基)-5-羟基-2-甲基四氢-2H-吡喃-3-基)氧基-4-羟基-2,4-二甲基四氢-2H-吡喃-3-基 3-甲基丁酸酯|CsnPharm

CAS No.: 16846-24-5

josamycin/交沙霉素 Catalog No. CSN21308

Synonyms: EN-141;Leucomycin V, 3-acetate 4B-(3-methylbutanoate);Leucomycin V

Josamycin is a macrolide antibiotic exhibiting antimicrobial activity against a wide spectrum of pathogens, such as bacteria. The dissociation constant Kd from ribosome for Josamycin is 5.5 nM.

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技术信息

生物活性

描述Josamycin is a macrolide antibiotic produced by Streptomyces narbonensis subsp. josamyceticus^[1]. It inhibits most strains of Mycoplasma pneumoniae, Streptococcus pneumoniae, and S. pyogenes at concentration of 0.5μg/mlin vitro. Corynebacterium diphtheriae, Neisseria meningitidis, N. gonorrheae, and Bordetella pertussis appear to be equally susceptible. A number of anaerobic bacteria, including Bacteroides fragilis, are susceptible to Josamycin at concentration of 2μg/ml^[2]. Most strains of Staphylococcus aureus are also susceptible to this antibiotic at concentration of 2μg/ml. Josamycin inhibits most erythromycin-resistant staphylococci. Unlike erythromycin, it does not induce macrolide resistance in these strains^[3]. Studies show that the average lifetime of ribosome is 3h when treated with Josamycin. The dissociation constants for Josamycin binding to ribosomes is 5.5nM. Josamycin slows down the formation of the first peptide bond to a nascent peptide in an amino acid-dependent way and completely inhibits formation of the second or third peptide bond, depending on peptide sequence at a saturating drug concentration, and synthesis of full length proteins is completely shut down by Josamycin at a saturating drug concentration.^[4]. This antibiotic had the highest distribution in the lung tissue in the animal after one-hour treatment^[5].
作用机制Josamycin block the entrance of nascent peptides to the peptide exit tunnel of the large ribosomal subunit.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00718705	Prematurity	Phase 3	Completed	-	France ... more >> Groupe Hospitalier Chenevier-Mondor, CHI Creteil, France, 94 Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2077 mL
- 6.0387 mL
- 12.0774 mL
- 5 mM
- 0.2415 mL
- 1.2077 mL
- 2.4155 mL
- 10 mM
- 0.1208 mL
- 0.6039 mL
- 1.2077 mL

技术信息

CAS号

16846-24-5

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C42H69NO15

运输

蓝冰

分子量

828.00

别名

EN-141;Leucomycin V, 3-acetate 4B-(3-methylbutanoate);Leucomycin V;3-acetate 4B-(3-methylbutanoate);Kitasamycin A3;Leucomycin A3;Turimycin A5;CCRIS 8511;交沙霉素

溶解度

DMSO	40.67 mg/mL (49.1 mM)

动物实验配方

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