| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
The primary targets of ceftiofur sodium are penicillin-binding proteins (PBPs) in the bacterial cell wall. By binding to PBPs, it inhibits the transpeptidase activity required for peptidoglycan cross-linking, leading to cell wall synthesis inhibition and bacterial cell death. It is resistant to many beta-lactamases due to its cephalosporin structure. It has broad-spectrum activity against Gram-positive and Gram-negative bacteria.
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| ln Vitro |
In vitro, ceftiofur sodium demonstrates broad-spectrum antibacterial activity against a wide range of Gram-positive and Gram-negative bacteria, including Pasteurella multocida, Mannheimia haemolytica, Histophilus somni, Actinobacillus pleuropneumoniae, Streptococcus species, and Escherichia coli. It has potent activity against respiratory pathogens in cattle and swine. Its in vitro activity has been characterized in MIC assays.
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| ln Vivo |
In vivo, ceftiofur sodium is used to treat respiratory diseases in cattle, swine, and horses, as well as foot rot, metritis, and other bacterial infections. It is administered by intramuscular or subcutaneous injection. It is the only cephalosporin approved for use in food-producing animals in the United States. Its efficacy has been demonstrated in numerous clinical field trials.
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| Enzyme Assay |
General protocols for antibacterial susceptibility testing use broth microdilution or agar dilution methods according to CLSI guidelines for veterinary pathogens. Bacterial strains (e.g., P. multocida, M. haemolytica, E. coli) are cultured overnight. Cultures are diluted and inoculated into 96-well plates containing serial dilutions of ceftiofur sodium (0.015-64 µg/mL). After incubation at 35-37°C for 16-20 hours, the MIC is determined. Quality control strains (e.g., E. coli ATCC 25922, S. aureus ATCC 29213) are included. MIC50 and MIC90 are calculated.
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| Cell Assay |
General protocols for cell-based studies of ceftiofur sodium are limited. The compound's primary mechanism of action is through bacterial cell wall synthesis inhibition. For studies on bacterial killing, bacterial cultures are treated with ceftiofur sodium at various concentrations (1-64x MIC) and incubated at 37°C. Bacterial viability is assessed by colony counting at various time points (0, 2, 4, 6, 24 hours). Time-kill curves are generated.
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| Animal Protocol |
General protocols for in vivo efficacy studies use animal models of respiratory disease (e.g., calves infected with P. multocida or M. haemolytica). Ceftiofur sodium is administered intramuscularly or subcutaneously at doses of 1-5 mg/kg daily for 3-5 days. Clinical signs (fever, respiratory rate, nasal discharge, cough) are scored. Bacterial counts in nasal swabs or lung tissue are determined. Body weight and feed intake are monitored. Survival rates are recorded.
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| ADME/Pharmacokinetics |
Ceftiofur sodium has a molecular weight of 545.56 g/mol (C19H16N5NaO7S3). It is a semi-synthetic third-generation cephalosporin. It is soluble in water. Following intramuscular or subcutaneous injection, it is rapidly absorbed and distributed to tissues. It is metabolized to desfuroylceftiofur, which is the active metabolite, and is excreted primarily via the kidneys. The elimination half-life is 2-5 hours depending on the species.
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| Toxicity/Toxicokinetics |
Ceftiofur sodium has a well-established safety profile in veterinary species. It may cause injection site reactions, pain, and swelling. Hypersensitivity reactions are rare. Withdrawal periods are required in food-producing animals to ensure that residues are below acceptable levels. It is not approved for human use and should not be used in humans.
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| Additional Infomation |
Ceftiofur sodium is an organic molecular entity. Ceftiofur sodium is the sodium salt form of ceftiofur, a semi-synthetic, β-lactamase-stable, broad-spectrum third-generation cephalosporin with antibacterial activity. Ceftiofur binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of bacterial cell walls. PBPs are enzymes involved in the final stages of bacterial cell wall assembly and in remodeling the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linking of peptidoglycan chains, which is essential for maintaining the strength and rigidity of bacterial cell walls. This leads to weakening of the bacterial cell wall and cell lysis. See also: Ceftiofur (containing the active ingredient). Indications: Swine: Treatment of bacterial respiratory diseases caused by Actinomyces pleuropneumoniae, Pasteurella multocida, Haemophilus parasuis, and Streptococcus suis. Treatment of septicemia, polyarthritis, or polyserositis caused by Streptococcus suis infection. Cattle: Treatment of acute interdigital necrosis (also known as hoof rot) in cattle. Treatment of acute postpartum (puerperal) metritis in cattle, applicable when other antimicrobial treatments are ineffective.
Ceftiofur sodium (CAS 104010-37-9) is a third-generation cephalosporin antibiotic used exclusively in veterinary medicine. It is used to treat respiratory diseases in cattle, swine, and horses, as well as foot rot and other infections. It is the only cephalosporin approved for use in food-producing animals in the United States. It is administered by injection and is not approved for human use. |
| Molecular Formula |
C19H16N5NAO7S3
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|---|---|
| Molecular Weight |
545.5444
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| Exact Mass |
545.01
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| CAS # |
104010-37-9
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| Related CAS # |
Ceftiofur;80370-57-6;Ceftiofur hydrochloride;103980-44-5;Ceftiofur-d3 sodium
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| PubChem CID |
23671563
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| Appearance |
White to light yellow solid powder
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| Density |
1.81g/cm3
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| LogP |
0.556
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
35
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| Complexity |
952
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| Defined Atom Stereocenter Count |
2
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| SMILES |
S1C([H])([H])C(C([H])([H])SC(C2=C([H])C([H])=C([H])O2)=O)=C(C(=O)[O-])N2C(C([H])([C@@]12[H])N([H])C(C(C1=C([H])SC(N([H])[H])=N1)=NOC([H])([H])[H])=O)=O.[Na+]
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| InChi Key |
RFLHUYUQCKHUKS-JUODUXDSSA-M
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| InChi Code |
InChI=1S/C19H17N5O7S3.Na/c1-30-23-11(9-7-34-19(20)21-9)14(25)22-12-15(26)24-13(17(27)28)8(5-32-16(12)24)6-33-18(29)10-3-2-4-31-10;/h2-4,7,12,16H,5-6H2,1H3,(H2,20,21)(H,22,25)(H,27,28);/q;+1/p-1/b23-11-;/t12-,16-;/m1./s1
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| Chemical Name |
sodium;(6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-(furan-2-carbonylsulfanylmethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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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) |
DMSO : ~50 mg/mL (~91.65 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (3.06 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 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. Solubility in Formulation 2: 1.67 mg/mL (3.06 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8330 mL | 9.1652 mL | 18.3305 mL | |
| 5 mM | 0.3666 mL | 1.8330 mL | 3.6661 mL | |
| 10 mM | 0.1833 mL | 0.9165 mL | 1.8330 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.