| 中文名称： | 达托霉素 | 中文别名： | 达托霉素 |
|---|---|---|---|
| 英文名称： | Daptomycin | CAS： | 103060-53-3 |
| 产品分类： | 原料 | 纯度： | 99.00% |
| 产品编号 | 品牌 | 纯度 | 规格 | 库存 | 价格 |
|---|---|---|---|---|---|
| R13359 | 瑞威尔 | 99.00% | 10g | 现货 | 2,500.00 元 |
| R13359 | 瑞威尔 | 99.00% | 50g | 99 | 11,500.00 元 |
| R13359 | 瑞威尔 | 99.00% | 100g | 99 | 22,000.00 元 |
| 标准名称: | 达帕托霉素 | 英文名称： | Daptomycin |
|---|---|---|---|
| CAS： | 103060-53-3 | 分子式： | C72H101N17O26 |
| 分子量： | 1620.67065787315 | 颜色与性状： | No data available |
| 密度： | 1.45 | 沸点： | 2078.2°C at 760 mmHg |
| 熔点： | 202-204°C | 水溶性： |
达托霉素物理化学性质
密度 1.5±0.1 g/cm3
沸点 2078.2±65.0 °C at 760 mmHg
熔点 202-204?C
分子式 C72H101N17O26
分子量 1620.671
闪点 1210.7±34.3 °C
精确质量 1619.710327
PSA 702.02000
LogP -4.07
外观性状 colorless to faint yellow
蒸汽压 0.0±0.3 mmHg at 25°C
折射率 1.638
储存条件 Store at -20°C
水溶解性 methanol: soluble5mg/mL
达托霉素生物活性
描述 Daptomycin 是一种脂肽类抗生素,具有体外快速杀除革兰氏阳性细菌的活性。
相关类别
信号通路 >> 抗感染 >> 细菌
研究领域 >> 感染
体外研究 达托霉素对萘夫西林敏感和耐药性葡萄球菌(MIC90小于或等于0.5 mg/L)和针对肠球菌(MIC90小于或等于2.0 mg/L)具有出色的体外抑制和杀菌活性。对于大多数分离的测试,达托霉素比万古霉素更有活性。除甲氧苄氨嘧啶-磺胺甲恶唑外,达托霉素是体外抗肠球菌最活跃的药物,对抗耐萘夫西林的葡萄球菌最活跃。当接种物从105 cfu/mL增加到107 cfu/mL时,达托霉素和万古霉素的MIC显着增加[1]。达托霉素在非常窄的药物浓度范围内(0.125至2.0 tLg/mL)有效,并且比其他针对粪链球菌的药物更具活性[2]。达托霉素抑制这些核苷酸连接的中间体的形成[3]。
体内研究 在每天两次给予10mg/kg的剂量时,与开始治疗后48小时内感染的未治疗对照相比,达托霉素显着减少了每个肾脏的生物体数量。每天给药一次20 mg/kg,达托霉素效果较差,但治疗4天后显着减少菌落数,其活性与万古霉素或万古霉素-庆大霉素相当,每日两次[2]。
动物实验 从18小时脑心浸液肉汤培养物制备含有109CFU / mL的接种物。随后通过标准的连续10倍稀释琼脂倾注平板技术测定每个接种物中的确切数量。用1.0-mL接种物静脉内攻击动物。已知该接种物感染正常大鼠的肾髓质。 24小时后，将动物分成8组，仅给予生理盐水（对照组）或用达托霉素10mg / kg（达托霉素10），达托霉素20mg / kg（达托霉素20），达托霉素10加庆大霉素开始抗生素治疗。 1.5mg / kg，20mg / kg的万古霉素，20mg / kg的万古霉素加1.5mg / kg的庆大霉素，每次注射30mg的氨苄青霉素，以及每只大鼠30mg的氨苄西林和1.5mg / kg的庆大霉素。动物每天一次接受达托霉素20;所有其他药物每天服用两次。皮下注射万古霉素和达托霉素;肌肉注射氨苄青霉素和庆大霉素。药物最多可使用13天。
参考文献
[1]. Benson CA, et al. Comparative in-vitro activity of LY146032 a new peptolide, with vancomycin and eight other agents against gram-positive organisms. J Antimicrob Chemother. 1987 Aug;20(2):191-6.
[2]. Miniter PM, et al. Activity of LY146032 in vitro and in experimental enterococcal pyelonephritis. Antimicrob Agents Chemother. 1987 Aug;31(8):1199-203.
[3]. Allen NE, et al. Inhibition of peptidoglycan biosynthesis in gram-positive bacteria by LY146032. Antimicrob Agents Chemother. 1987 Jul;31(7):1093-9.
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