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Ceftizoxime sodium (SKF-88373) Sale

(Synonyms: 头孢唑肟钠; SKF-88373) 目录号 : GC32180

A cephalosporin antibiotic

Ceftizoxime sodium (SKF-88373) Chemical Structure

Cas No.:68401-82-1

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产品描述

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)

Chemical Properties

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.
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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。
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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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Research Update

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.