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| Targets |
Cefquinome Sulfate targets bacterial penicillin-binding proteins (PBPs), which are enzymes involved in the terminal stages of assembling the bacterial cell wall. By binding to these PBPs, cefquinome inhibits the cross-linking of peptidoglycan, a key component of the bacterial cell wall. This leads to cell lysis and death. Its high stability against beta-lactamases makes it effective against resistant bacteria.
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| ln Vitro |
In vitro, cefquinome sulfate demonstrates broad-spectrum antibacterial activity against a range of Gram-positive and Gram-negative bacteria. Its activity is assessed using standard susceptibility testing methods, such as broth dilution or disk diffusion assays, to determine the minimum inhibitory concentration (MIC). Its high potency and stability against beta-lactamases contribute to its effectiveness.
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| ln Vivo |
In vivo, cefquinome sulfate is used in veterinary medicine for the treatment of bacterial infections in cattle, pigs, poultry, and other animals. It is effective against a wide range of pathogens, including those responsible for respiratory and systemic infections. Its high cellular penetration and stability against beta-lactamases contribute to its in vivo efficacy.
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| Enzyme Assay |
The in vitro antibacterial activity of cefquinome sulfate is assessed using standard susceptibility testing methods, such as broth dilution or disk diffusion assays. These assays measure the minimum inhibitory concentration (MIC) against various bacterial strains. Its stability against beta-lactamases can be assessed using enzymatic assays. These methods are used to characterize the compound's antibacterial spectrum and potency.
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| Cell Assay |
In vitro cellular assays for cefquinome sulfate are not typically conducted, as it is an antibiotic that targets bacteria rather than eukaryotic cells. Its activity is assessed in bacterial cultures rather than mammalian cell lines. However, its effects on bacterial cell viability and growth are measured using standard microbiological techniques.
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| Animal Protocol |
In vivo animal studies for cefquinome sulfate have been conducted in veterinary species to evaluate its efficacy and safety. These studies typically involve administering the compound to animals with induced or naturally occurring infections and measuring clinical outcomes, bacterial clearance, and pharmacokinetic parameters. Its efficacy has been established in various veterinary indications.
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| ADME/Pharmacokinetics |
Cefquinome sulfate is administered parenterally in veterinary medicine. Its pharmacokinetic properties are characterized by good tissue distribution and a relatively long half-life, allowing for once-daily or twice-daily dosing. It is excreted primarily by the kidneys. Its high cellular penetration contributes to its efficacy against intracellular pathogens.
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| Toxicity/Toxicokinetics |
Cefquinome sulfate is generally well-tolerated in animals. Adverse effects are uncommon but may include local reactions at the injection site and, rarely, hypersensitivity reactions. As with other cephalosporins, it should be used with caution in animals with a history of penicillin allergy. Its safety profile has been established in veterinary use.
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| References | |
| Additional Infomation |
Cefquinoline sulfate is the sulfate form of cefaquinoline, a semi-synthetic, broad-spectrum fourth-generation aminothiazole cephalosporin with antibacterial activity. Ceffaquinoline 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 crucial for maintaining the strength and rigidity of the bacterial cell wall. This leads to weakening of the bacterial cell wall, ultimately resulting in cell lysis.
Cefquinome Sulfate is a fourth-generation cephalosporin antibiotic used in veterinary medicine. It is characterized by high cellular penetration and high stability against beta-lactamases. It acts by inhibition of bacterial cell wall synthesis and is effective against a wide range of pathogens. It is marketed for the treatment of bacterial infections in animals. |
| Molecular Formula |
C23H24N6O5S2.H2SO4
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|---|---|
| Molecular Weight |
626.68
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| Exact Mass |
626.092
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| CAS # |
118443-89-3
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| Related CAS # |
Cefquinome;84957-30-2
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| PubChem CID |
5488763
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
1.676
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
41
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| Complexity |
1050
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C1[C@@H](NC(/C(C2=CSC(N)=N2)=N\OC)=O)[C@@]3([H])SCC(C[N+]4=C5CCCCC5=CC=C4)=C(C(O)=O)N13.[O-]S(=O)(O)=O
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| InChi Key |
KYOHRXSGUROPGY-WVEKLOCCSA-N
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| InChi Code |
InChI=1S/C23H24N6O5S2.H2O4S/c1-34-27-16(14-11-36-23(24)25-14)19(30)26-17-20(31)29-18(22(32)33)13(10-35-21(17)29)9-28-8-4-6-12-5-2-3-7-15(12)28;1-5(2,3)4/h4,6,8,11,17,21H,2-3,5,7,9-10H2,1H3,(H3-,24,25,26,30,32,33);(H2,1,2,3,4)/b27-16+;/t17-,21-;/m1./s1
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| Chemical Name |
(6R,7R)-7-[[(2E)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-8-oxo-3-(5,6,7,8-tetrahydroquinolin-1-ium-1-ylmethyl)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate;sulfuric acid
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~125 mg/mL (~199.46 mM)
H2O : ~2 mg/mL (~3.19 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.32 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.32 mM) (saturation unknown) 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. 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 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 | 1.5957 mL | 7.9786 mL | 15.9571 mL | |
| 5 mM | 0.3191 mL | 1.5957 mL | 3.1914 mL | |
| 10 mM | 0.1596 mL | 0.7979 mL | 1.5957 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.
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