| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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| Other Sizes |
| Targets |
Bacterial cell wall synthesis; β-lactam
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| ln Vitro |
MIC for cefotaxime sodium against V. vulnificus CMCP6 is 0.0625 mg/L[4]. - The minimum inhibitory concentration (MIC) of cefotaxime against V. vulnificus CMCP6 was determined to be 0.0625 mg/L using the microdilution method according to CLSI guidelines [1].
The MIC of cefotaxime against V. vulnificus MO6-24/O was also 0.0625 mg/L [1]. - In time-kill assays using 3/4 MIC concentrations, cefotaxime alone showed moderate bactericidal activity against V. vulnificus CMCP6 [1]. The combination of cefotaxime with ciprofloxacin demonstrated synergistic bactericidal activity, with bacterial colony counts after 24 h of in vitro treatment being lower for the combination than for cefotaxime, ciprofloxacin, minocycline, or cefotaxime-plus-minocycline [1]. - At sub-inhibitory concentrations (1/4 MIC), cefotaxime had a modest inhibitory effect on V. vulnificus cytotoxicity for HeLa cells and on rtxA1 transcription, but was significantly less effective than ciprofloxacin (P < 0.05 for both comparisons) [1]. |
| ln Vivo |
Compared to earlier regimens, the combination of ciprofloxacin and cefotaxime is more effective in eliminating V. vulnificus in vivo[4].- In a mouse model of V. vulnificus sepsis using an initial inoculum of 1×108 cfu, treatment with cefotaxime alone (30 mg/kg i.p. every 6 h for 42 h) resulted in a 96-h survival rate of 0% (0/20), which was significantly lower than the 85% (17/20) survival rate observed with the cefotaxime-plus-ciprofloxacin combination (P < 0.001) [1].
The survival rate in the cefotaxime-plus-minocycline group was 35% (7/20) [1]. - Using a lower initial inoculum of 1×107 cfu, all mice treated with cefotaxime alone (n=12) survived for 96 h, similar to other treatment groups [1]. However, bacterial counts in the liver and spleen at 24 and 48 h after treatment initiation were significantly higher in the cefotaxime monotherapy group compared to the cefotaxime-plus-ciprofloxacin group: liver at 24 h (19,544 ± 12,097 vs. 473 ± 309 CFU/g, P < 0.001), liver at 48 h (9,216 ± 101 vs. 162 ± 35 CFU/g, P < 0.001), spleen at 24 h (13,180 ± 5,558 vs. 1,813 ± 6,514 CFU/g, P < 0.001), and spleen at 48 h (1,304 ± 565 vs. 217 ± 87 CFU/g, P < 0.001) [1]. |
| Cell Assay |
- Cytotoxicity assay (LDH release): HeLa cells were seeded in 48-well plates and cultured for 24 h [1].
Overnight-cultured V. vulnificus (MO6-24/O) were re-suspended in PBS after logarithmic growth [1]. HeLa cells (2×105 cells/mL) were infected with V. vulnificus (5×105 cfu/mL) in the presence or absence of 1/4 MIC of cefotaxime, minocycline, or ciprofloxacin for 120 min [1]. Cytotoxicity was measured by assaying lactate dehydrogenase (LDH) released into the supernatant using a commercial kit [1]. The impaired cytotoxicity of the rtxA1 deletion mutant (CMM770) compared to the wild-type strain confirmed that cytotoxicity at 120 min was mainly due to RtxA1 [1]. At 1/4 MIC, cefotaxime inhibited V. vulnificus-induced cytotoxicity less effectively than ciprofloxacin (P < 0.05) [1]. - Transcriptional reporter assay (β-galactosidase): A chromosomal PrtxA1:lacZ transcriptional reporter strain of V. vulnificus MO6-24/O was constructed [1]. An overnight culture of the reporter strain was inoculated into HI broth at 5×105 cfu/mL with or without 1/4 MICs of antibiotics for 120 min [1]. The culture was lysed, and β-galactosidase activity was measured using a substrate containing O-nitrophenyl-β-D-galactopyranoside [1]. At 1/4 MIC, cefotaxime inhibited rtxA1 transcription less effectively than ciprofloxacin (P < 0.05) [1]. |
| Animal Protocol |
- Female, 8-week-old BALB/c mice (average weight 20 g) were used [1].
To induce iron overload, 900 μg ferric ammonium citrate was administered intraperitoneally 30 min before V. vulnificus inoculation [1]. Mice were inoculated subcutaneously over the right thigh with either 1×107 or 1×108 cfu of V. vulnificus CMCP6 [1]. Antibiotic therapy was initiated 2 h after inoculation [1]. Cefotaxime was administered intraperitoneally at 30 mg/kg body weight every 6 h [1]. All antibiotics were given for a total of 42 h [1]. Control mice received 0.1 mL sterile saline every 6 h [1]. For survival studies, animals were monitored every 6 h, and humane endpoints were used based on a clinical scoring system (combined score ≥8) according to KFDA guidelines [1]. For bacterial clearance studies, mice were euthanized at 24 and 48 h after treatment initiation; livers and spleens were homogenized, serially diluted, and plated onto Brain-Heart infusion agar for CFU quantification [1]. Animal Model: 8-week-old female BALB/c mice that are free of a particular pathogen[4]. Dosage: 30 mg/kg. Administration: IP every 6 h. Result: Mice treated with cefotaxime-plus-ciprofloxacin had fewer viable bacterial counts in their livers than mice treated with cefotaxime alone (P<0.001 at 24 and 48 hours, respectively). |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Rapidly absorbed following intramuscular injection. Approximately 20-36% of an intravenously administered dose of 14C-cefotaxime is excreted by the kidney as unchanged cefotaxime and 15-25% as the desacetyl derivative, the major metabolite. Metabolism / Metabolites Approximately 20-36% of an intravenously administered dose of 14C-cefotaxime is excreted by the kidney as unchanged cefotaxime and 15-25% as the desacetyl derivative, the major metabolite. The desacetyl metabolite has been shown to contribute to the bactericidal activity. Two other urinary metabolites (M2 and M3) account for about 20-25%. They lack bactericidal activity. Biological Half-Life Approximately 1 hour. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Cefotaxime has been discontinued in the United States. Limited information suggests that cefotaxime concentrations in breast milk are low and are not expected to have adverse effects on breastfed infants. There have been reports that cephalosporins occasionally disrupt the infant's gut microbiota, leading to diarrhea or thrush, but these effects have not been fully assessed. Cefotaxime is safe for use by breastfeeding women. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. |
| References |
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| Additional Infomation |
Cefotaxime sodium is a cephalosporin organosodium salt with acetoxymethyl and [2-(2-amino-1,3-thiazolyl-4-yl)-2-(methoxyimino)acetyl]amino side groups. It contains a cefotaxime (1-) group. Cefotaxime sodium is the sodium salt form of cefotaxime, a third-generation β-lactam cephalosporin antibiotic with bactericidal activity. Cefotaxime sodium binds to and inactivates penicillin-binding protein (PBP) located on the inner membrane of bacterial cell walls. Inactivation of PBP interferes with the cross-linking of peptidoglycan chains, which is crucial for maintaining the strength and rigidity of bacterial cell walls. This leads to weakening of the bacterial cell wall and ultimately cell lysis. Compared to second- and first-generation cephalosporins, cefotaxime sodium exhibits stronger activity against Gram-negative bacteria and weaker activity against Gram-positive bacteria. Semi-synthetic broad-spectrum cephalosporins. See also: Cefotaxime (containing the active fraction).
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| Molecular Formula |
C16H16N5NAO7S2
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|---|---|
| Molecular Weight |
477.4473
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| Exact Mass |
477.038
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| Elemental Analysis |
C, 40.25; H, 3.38; N, 14.67; Na, 4.82; O, 23.46; S, 13.43
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| CAS # |
64485-93-4
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| Related CAS # |
Cefotaxime;63527-52-6;Cefotaxime-d3 sodium; Cefotaxime sodium;64485-93-4; 63527-52-6 (free); 66340-28-1; 66340-33-8
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| PubChem CID |
10695961
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| Appearance |
White to off-white solid powder
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| Density |
1.8 g/cm3
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| Melting Point |
162-163ºC(lit.)
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| Index of Refraction |
61 ° (C=1， H2O)
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
839
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| Defined Atom Stereocenter Count |
2
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| SMILES |
S1C([H])([H])C(C([H])([H])OC(C([H])([H])[H])=O)=C(C(=O)[O-])N2C([C@]([H])([C@@]12[H])N([H])C(/C(/C1=C([H])SC(N([H])[H])=N1)=N/OC([H])([H])[H])=O)=O.[Na+]
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| InChi Key |
AZZMGZXNTDTSME-JUZDKLSSSA-M
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| InChi Code |
InChI=1S/C16H17N5O7S2.Na/c1-6(22)28-3-7-4-29-14-10(13(24)21(14)11(7)15(25)26)19-12(23)9(20-27-2)8-5-30-16(17)18-8;/h5,10,14H,3-4H2,1-2H3,(H2,17,18)(H,19,23)(H,25,26);/q;+1/p-1/b20-9-;/t10-,14-;/m1./s1
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| Chemical Name |
sodium;(6R,7R)-3-(acetyloxymethyl)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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| Synonyms |
Cefotaxime Sodium; CEFOTAXIME SODIUM SALT; Cefotaxim sodium salt; Cefotax; CHEBI:3498; Merck Brand of Cefotaxime Sodium; Pisa Brand of Cefotaxime Sodium; Primafen; Ru 24756; Ru-24756; Ru24756; Sodium, Cefotaxime; Taporin; Viken Brand of Cefotaxime Sodium;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : 50~95 mg/mL (104.72~198.97 mM )
DMSO : ~45 mg/mL (~94.25 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.36 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.08 mg/mL (4.36 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: 10% DMSO+90% Corn Oil: ≥ 2.5 mg/mL (5.24 mM) Solubility in Formulation 5: 100 mg/mL (209.45 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0945 mL | 10.4723 mL | 20.9446 mL | |
| 5 mM | 0.4189 mL | 2.0945 mL | 4.1889 mL | |
| 10 mM | 0.2094 mL | 1.0472 mL | 2.0945 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Effect of Administration of 3rd Generation Cephalosporin on the Digestive Carrying of 3rd Generation Cephalosporin-resistant Enterobacteriaceae (CEF-IMPACT)
CTID: NCT03922919
Phase: Phase 4 Status: Unknown status
Date: 2019-04-22
Products are for research use only; We do not sell to patients
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