|(6R,7R)-7-((Z)-2-(2-氨基噻唑-4-基)-2-(甲氧基亚氨基)乙酰氨基)-3-((2-(2-羟乙基)-3-亚氨基-2,3-二氢-1H-吡唑-1-基)甲基)-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-甲酸硫酸盐(1:1)|CsnPharm

CAS No.: 122841-12-7

Cefoselis sulfate/硫酸头孢噻利 Catalog No. CSN10577

Synonyms: FK-037;FK 037 Sulfate;Cefoselis (sulfate)

Cefoselis Sulfate is a semisynthetic, broad-spectrum, β-lactamase-resistant, fourth-generation cephalosporin with antibacterial activity.

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400-920-2911

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技术信息

生物活性

描述Cefoselis (Sulfate) is a widely used beta-lactam antibiotic, but occasionally induces seizures and convulsion in elder and renal failure patients. Cefoselis was dose-dependently appeared in brain extracellular fluid in proportion to its blood level. A local administration of cefoselis into the hippocampus through the microdialysis probe caused a striking elevation of extracellular glutamate, with a minimum increase in gamma-aminobutyric acid (GABA)^[3]. Cefoselis showed poor activity against extended-spectrum β-lactamase (ESBL)-producing Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis, with susceptibility rates of < 10% each, while the susceptibility rates of this antibiotic against non-ESBL-producing strains of these organisms were 100%, 94.3%, and 97.0%, respectively. Cefoselis exhibited susceptibility rates of 56.7-83.3% against other tested Enterobacteriaceae isolates^[4].
参考文献

[1] Ohtaki K, Matsubara K, et al. Cefoselis, a beta-lactam antibiotic, easily penetrates the blood-brain barrier and causes seizure independently by glutamate release. J Neural Transm (Vienna). 2004 Dec;111(12):1523-35.
[2] Sugimoto M, Fukami S, et al. The beta-lactam antibiotics, penicillin-G and cefoselis have different mechanisms and sites of action at GABA(A) receptors. Br J Pharmacol. 2002 Jan;135(2):427-32.
[3] Ohtaki K, Matsubara K, Fujimaru S, Shimizu K, Awaya T, Suno M, Chiba K, Hayase N, Shiono H. Cefoselis, a beta-lactam antibiotic, easily penetrates the blood-brain barrier and causes seizure independently by glutamate release. J Neural Transm (Vienna). 2004 Dec;111(12):1523-35.
[4] Cheng JW, Su JR, Xiao M, Yu SY, Zhang G, Zhang JJ, Yang Y, Duan SM, Kudinha T, Yang QW, Xu YC. In vitro Activity of a New Fourth-Generation Cephalosporin, Cefoselis, Against Clinically Important Bacterial Pathogens in China. Front Microbiol. 2020 Feb 28;11:180.

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
- 1.6112 mL
- 8.0562 mL
- 16.1125 mL
- 5 mM
- 0.3222 mL
- 1.6112 mL
- 3.2225 mL
- 10 mM
- 0.1611 mL
- 0.8056 mL
- 1.6112 mL

技术信息

CAS号

122841-12-7

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H24N8O10S3

运输

蓝冰

分子量

620.64

别名

FK-037;FK 037 Sulfate;Cefoselis (sulfate);Winsef;(6R(6alpha7beta(Z)))7(((2Amino4thiazolyl)(methoxyimino)acetyl)amino)3((23dihydro2(2hydroxyethyl)3imino1Hpyrazol1yl)methyl)8oxo5Thia1azabicyclo(4.2.0)oct2ene2carboxylic acid sulfate;硫酸头孢噻利;头孢西利硫酸盐

溶解度

DMSO	3.0 mg/mL (4.8 mM)
Ethanol	Insoluble

动物实验配方

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Cefoselis sulfate/硫酸头孢噻利 Catalog No. CSN10577

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