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Cefoselis sulfate

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Chemical Structure| 122841-12-7 同义名 : FK-037;Cefoselis (sulfate);FK 037 Sulfate
CAS号 : 122841-12-7
货号 : A124704
分子式 : C19H24N8O10S3
纯度 : 98%
分子量 : 620.636
MDL号 : MFCD01940015
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(169.18 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 14 mg/mL(22.56 mM)，配合低频超声助溶
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.61mL

0.32mL

0.16mL

8.06mL

1.61mL

0.81mL

16.11mL

3.22mL

1.61mL
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.