S-(-)-Cefotaxime | 1151540-28-1

• 物质功能分类: 原料药 - 抗生素类药物 - 头孢菌素类药
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: S-(-)-Cefotaxime
• 英文别名: (6S,7S)-3-(acetyloxymethyl)-7-[[(2E)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
• CAS: 1151540-28-1；63527-52-6
• 化学式: C₁₆H₁₇N₅O₇S₂
• 分子量: 455.5
• InChiKey: GPRBEKHLDVQUJE-ZLWRGHKMSA-N

物化性质

• 熔点：
  >158°C (dec.)
• 密度：
  1.80±0.1 g/cm3(Predicted)
• 溶解度：
  可溶于DMSO（少许）、甲醇（少许）
• LogP：
  1.2

计算性质

• 辛醇/水分配系数(LogP)：
  -1.4
• 重原子数：
  30
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  227
• 氢给体数：
  3
• 氢受体数：
  12

安全信息

• 海关编码：
  3003201100

制备方法与用途

生物活性

Cefotaxime是第三代头孢菌素抗生素，对革兰氏阴性菌和阳性菌具有广谱活性。

体外研究

Cefotaxime exhibits an MIC of 0.0625 mg/L for V. vulnificus CMCP6.

体内研究

The combination of ciprofloxacin and cefotaxime is more effective in clearing V. vulnificus in vivo than previously used regimens.

Animal Model:	Female, specific pathogen free, 8-week-old BALB/c mice.
Dosage:	30 mg/kg.
Administration:	IP every 6 h.
Result:	The viable bacterial counts in liver were lower in mice treated with cefotaxime-plus-ciprofloxacin than in those treated with cefotaxime alone (P<0.001 at 24 h and 48 h, each).

化学性质 

白色粉末。熔点162-163℃（分解）。易溶于水。稀溶液无色或微黄色，浓度较高时呈灰黄色。变质时呈深黄色或棕色。

用途 

半合成肟型头孢菌素，为第三代头孢菌素。本品对革兰阴性菌、尤其对肠杆菌作用强大。主要用于敏感菌所致呼吸系统感染，泌尿系统感染，胆道及肠道感染，皮肤及软组织感染，烧伤和骨关节感染等。

用途 

用作抗菌药，属半合成肟型头孢菌素

生产方法 

以发酵生产的头孢菌素C为原料，经裂解得7-氨基头孢烷酸（7-ACA），再经硅酯化，与侧链酸缩合、水解、结晶得头孢噻肟，再与醋酸钠成盐，经脱色、无菌过滤、结晶得到头孢噻肟（钠盐）成品。

文献信息

• Compounds and Methods for modulating the Silencing of a Polynucleotide of Interest
  申请人：Peng Jin

  公开号：US20090306035A1

  公开（公告）日：2009-12-10

  Methods and compositions comprising chemical compounds that modulate the silencing of a polynucleotide of interest in a cell are provided. Such chemical compounds when used in combination with an appropriate silencing element can be used to modulate (increase or decrease) the level of the polynucleotide targeted by the silencing element. Methods of using such compositions both in therapies involving RNAi-mediated suppression of gene expression, as well as, in vitro methods that allow for the targeted modulation of expression of a polynucleotide of interest are provided. Pharmaceutical or cosmetic formulations comprising such compounds and silencing elements also are disclosed. Methods for screening a compound of interest for the ability to modulate the activity of a heterologous silencing element also are provided.