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| 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]. |
| Concentration | Treated Time | Description | References | |
| Fusobacterium nucleatum | 0.01 mg/mL | 3.5 h or 24 h | Construct phenotypic fingerprints via flow cytometry to predict the mechanism of action of cephalothin. Results showed that the mechanism of action of cephalothin was successfully predicted as the 'Cell Wall Synthesis' class. | Microbiol Spectr. 2024 Apr 2;12(4):e0393123 |
| Actinomyces viscosus | 0.01 mg/mL | 3.5 h or 24 h | Construct phenotypic fingerprints via flow cytometry to predict the mechanism of action of cephalothin. Results showed that the mechanism of action of cephalothin was successfully predicted as the 'Cell Wall Synthesis' class. | Microbiol Spectr. 2024 Apr 2;12(4):e0393123 |
| Bordetella bronchiseptica | 32 μg/ml | 16 to 20 h | To determine the antimicrobial activity of cephalothin against Bordetella bronchiseptica isolates from swine respiratory tract infections, showing that the MIC90 was 32 μg/ml. | Antimicrob Agents Chemother. 2004 Dec;48(12):4903-6 |
| Coagulase-negative staphylococci (CoNS) | 0.125 to 1026 mg/L | Overnight incubation | Evaluated the synergy of cephalothin with amikacin, showing synergistic effect in 26.9% and partially synergistic in 73.07% of isolates | Ann Clin Microbiol Antimicrob. 2006 Oct 12;5:25 |
| Methicillin-resistant Staphylococcus aureus (MRSA) | 0.125 to 1026 mg/L | Overnight incubation | Evaluated the synergy of cephalothin with amikacin, showing synergistic effect in 26.9% and partially synergistic in 73.07% of isolates | Ann Clin Microbiol Antimicrob. 2006 Oct 12;5:25 |
| Administration | Dosage | Frequency | Description | References | ||
| Insect larvae (Galleria mellonella) | MRSA-infected insect larva model | Injection | 30 mg/kg | Every 6 hours for up to 84 hours | To evaluate the combined therapeutic effect of Cephalothin with the quorum-sensing inhibitor F12, results showed that combination therapy significantly increased the survival time of MRSA-infected insect larvae. | Antimicrob Agents Chemother. 2015 Mar;59(3):1512-8 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.61mL 2.52mL 1.26mL |
25.22mL 5.04mL 2.52mL |
|
| CAS号 | 153-61-7 |
| 分子式 | C16H16N2O6S2 |
| 分子量 | 396.44 |
| SMILES Code | O=C(C(N12)=C(COC(C)=O)CS[C@]2([H])[C@H](NC(CC3=CC=CS3)=O)C1=O)O |
| MDL No. | MFCD00242614 |
| 别名 | Cephalotin; Cephalothinum; Spaly Brand of Cephalothin Sodium; Sodium Cephalothin; Seffin; Salt, Cephalothin Monosodium; Normon Brand of Cephalothin Sodium; Monosodium Salt, Cephalothin; Cefalotina; Cefalothin; Cefalotin; Cephalotin acid |
| 运输 | 蓝冰 |
| InChI Key | XIURVHNZVLADCM-IUODEOHRSA-N |
| Pubchem ID | 6024 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, room temperature |
| 溶解方案 |
DMSO: 105 mg/mL(264.86 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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