|(6R,7R)-3-(乙酰氧基甲基)-8-氧代-7-(2-(噻吩-2-基)乙酰氨基)-5-噻吩-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸|CsnPharm

CAS No.: 153-61-7

Cephalothin/头孢噻吩 Catalog No. CSN23657

Synonyms: Cephalotin;Cephalotin acid;Cefalotin

Cephalothin is a cephalosporin antibiotic with antibacterial activity.

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技术信息

生物活性

描述Cephalotin (Cephalotin) is a beta-lactam antibiotic, inhibits class C β-lactamase AmpC, with an Ki of 0.32 µM^[1]. The maximum plasma cephalothin concentration after IM administration was 11.3 +/- 3.71 micrograms/ml. The terminal half-life was 47.0 minutes and was longer than the half-life after IV administration. The bioavailability of cephalothin given IM ranged from 38.3% to 93.1% and averaged 65.0 +/- 20.5%^[2]. Two derivatives of cephalothin, compound I and II, were synthesized and demonstrated strong growth inhibition of ampicillin resistant Escherichia coli (E. coli). The MIC50 of I and II were determined to be 55 microg/mL and 30 microg/mL, respectively. Cephalothin showed less than 20% growth inhibition of E. coli at all concentrations based on assay of colony forming units. Compounds I and II showed greater than 50% growth inhibition of E. coli at all concentrations greater than 50 microg/mL (more than 65% at 400 microg/mL)^[3]. Patients receiving intravenous sodium cephalothin or intravenous penicillin-G. Immunogenicity was indicated by a higher incidence of anti-cephalothin antibody in patients after having received the drug than in controls and by an increase in titre of anti-cephalothin antibody during administration of the drug. Further, patients receiving cephalothin had a high incidence of anti-penicillin antibodies and the anti-penicillin antibody titre increased during cephalothin administration^[4].
参考文献

[1] Morandi S, Morandi F, Caselli E, Shoichet BK, Prati F. Structure-based optimization of cephalothin-analogue boronic acids as beta-lactamase inhibitors. Bioorg Med Chem. 2008;16(3):1195‐1205
[2] Ruoff WW Jr, Sams RA. Pharmacokinetics and bioavailability of cephalothin in horse mares. Am J Vet Res. 1985;46(10):2085‐2090
[3] Bartzatt R, Cirillo SL, Cirillo JD. Derivatives of cephalothin that inhibit ampicillin resistant Escherichia coli. Med Chem. 2007;3(1):45‐49
[4] Abraham GN, Petz LD, Fudenberg HH. Immunohaematological cross-allergenicity between penicillin and cephalothin in humans. Clin Exp Immunol. 1968;3(4):343‐357

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
- 2.5224 mL
- 12.6122 mL
- 25.2245 mL
- 5 mM
- 0.5045 mL
- 2.5224 mL
- 5.0449 mL
- 10 mM
- 0.2522 mL
- 1.2612 mL
- 2.5224 mL

技术信息

CAS号

153-61-7

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H16N2O6S2

运输

蓝冰

分子量

396.44

别名

Cephalotin;Cephalotin acid;Cefalotin;Cefalothin;Cefalotina;Monosodium Salt;Salt;Seffin;头孢噻吩

溶解度

DMSO	77.0 mg/mL (194.2 mM)

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