Cephalothin

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Chemical Structure| 153-61-7 同义名 : 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
CAS号 : 153-61-7
货号 : A437484
分子式 : C16H16N2O6S2
纯度 : 97%
分子量 : 396.438
MDL号 : MFCD00242614
存储条件：

Pure form Keep in dark place,Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
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].
实验方案
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
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