Ceftizoxime sodium (SKF-88373)
(Synonyms: 头孢唑肟钠; SKF-88373) 目录号 : GC32180A cephalosporin antibiotic
Cas No.:68401-82-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
- Datasheet
Ceftizoxime is a cephalosporin antibiotic.1 Ceftizoxime is active against clinical isolates of the Gram-positive bacteria S. aureus, S. pyogenes, and S. epidermidis (IC50s = 1.56, ≤0.025, and 0.78 ?g/ml, respectively), as well as clinical isolates of the Gram-negative bacteria E. coli, K. pneumoniae, and P. mirabilis (IC50s = 0.1, ≤0.025, and ≤0.025 ?g/ml, respectively). It is protective against S. aureus, E. coli, P. mirabilis, or P. vulgaris infection in mice (ED50s = 4.03, 0.02, 0.255, and 0.038 mg/kg, respectively).2 Formulations containing ceftizoxime have been used in the treatment of a variety of bacterial infections.
1.Kamimura, T., Matsumoto, Y., Okada, N., et al.Ceftizoxime (FK 749), a new parenteral cephalosporin: In vitro and in vivo antibacterial activitiesAntimicrob. Agents Chemother.16(5)540-548(1979) 2.Nishida, M., Kamimura, T., Okada, N., et al.Comparison of antibacterial activity of a new cephalosporin, ceftizoxime (FK 749) with other cephalosporin antibioticsJ. Antibiot. (Tokyo)32(12)1319-1327(1979)
Cas No. | 68401-82-1 | SDF | |
别名 | 头孢唑肟钠; SKF-88373 | ||
Canonical SMILES | O=C(C(N12)=CCS[C@]2([H])[C@H](NC(/C(C3=CSC(N)=N3)=N\OC)=O)C1=O)[O-].[Na+] | ||
分子式 | C13H12N5NaO5S2 | 分子量 | 405.38 |
溶解度 | DMSO : 15 mg/mL (37.00 mM) | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.4668 mL | 12.3341 mL | 24.6682 mL |
5 mM | 0.4934 mL | 2.4668 mL | 4.9336 mL |
10 mM | 0.2467 mL | 1.2334 mL | 2.4668 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Toxicity and reproduction studies of Ceftizoxime sodium
Arzneimittelforschung 1980;30(10):1669-79.PMID:6933994doi
Sodium (6R,7R)-7-[(Z)-2-(2-amino-4-thiazoyl)-methoxyiminoacetamido]-8-oxo-5-thia-1-azabicyclo[4,2,0] oct-2-ene-2-carboxylate (Ceftizoxime sodium), a new semisynthetic cephalosporin derivative, was tested for acute toxicity in various laboratory animal species, nephrotoxicity in rabbits, subacute and chronic toxicity in rats and dogs, and effect on fertility and teratogenicity in rats and rabbits. The i.v. LD50 values of Ceftizoxime sodium in mice and rats were around 6000 mg/kg, and no deaths occurred in dogs after the largest dose of 3200 mg/kg. There was no evidence of nephrotoxicity of Ceftizoxime sodium in rabbits after an i.v. dose of 1000 mg/kg. Clear-cut changes in subacute and chronic toxicity studies of Ceftizoxime sodium were local damage at the injection site and its secondary reactions, although reversible peripheral anemia was observed in one female dog given 1000 mg/kg i.v. In the reproduction studies, Ceftizoxime sodium had no adverse effects on fertility or fetal development in rats or rabbits.
Human serum paraoxonase-1 (hPON1): in vitro inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and Ceftizoxime sodium
J Enzyme Inhib Med Chem 2015;30(4):622-8.PMID:25519764DOI:10.3109/14756366.2014.959511.
In this study, we investigated the effects of antibacterial drugs (moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and Ceftizoxime sodium) on human serum paraoxonase-1 (hPON1) enzyme activity from human serum in vitro conditions. For this purpose, hPON1 enzyme was purified from human serum using simple chromatographic methods. The antibacterial drugs exhibited inhibitory effects on hPON1 at low concentrations. Ki constants were calculated to be 2.641 ± 0.040 mM, 5.525 ± 0.817 mM, 35.092 ± 1.093 mM, 252.762 ± 5.749 mM and 499.244 ± 10.149 mM, respectively. The inhibition mechanism of moxifloxacin hydrochloride was competitive, whereas levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and Ceftizoxime sodium were noncompetitive inhibitors.
Structural identification and characterization of impurities in Ceftizoxime sodium
J Pharm Biomed Anal 2007 Jan 17;43(2):733-40.PMID:16950586DOI:10.1016/j.jpba.2006.07.031.
Ceftizoxime sodium is a parenteral beta-lactamic antibacterial drug. In the synthesis of Ceftizoxime sodium, eight process related impurities were detected in HPLC analysis. Pure impurities obtained by both synthesis and preparative HPLC were co-injected with ceftizoxime sample to confirm the retention times in HPLC. The impurities were characterized as, (6R,7R)-7-amino-3-cephem-4-carboxylic acid (impurity I); (6R,7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-(methoxyimino)acetamido]-3-cephem-1-oxo-4-carboxylic acid (impurity II); (4RS,6R,7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-(methoxyimino) acetamido]-3,4-dihydro-3-cephem-4-carboxylic acid (impurity III); (6R,7R)-7-[(E)-2-(2-amino-4-thiazolyl)-2-(methoxyimino)acetamido]-3-cephem-4-carboxylic acid (impurity IV); (6R,7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-(methoxyimino)acetamido]-3-cephem-N-(3-cephem-4-carboxy-7-yl)-4-carboxamide (impurity V); (6R,7R)-7-[(Z)-2-[[(Z)-2-(2-amino-4-thiazolyl)-2-(methoxyimino)acetylamino]thiazol-4-yl]-2-methoxyiminoacetamido]-3-cephem-4-carboxylic acid (impurity VI); 2-mercaptobenzothiazole (impurity VII) and 2-mercapto benzothiazolyl [(Z)-2-(2-amino-4-thiazolyl)-2-methoxyimino] acetate (impurity VIII). Structural elucidation of all impurities by spectral data ((1)H NMR, (13)C NMR, MS and IR) has been discussed.