| Size | Price | Stock | Qty |
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| 10mg |
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| Targets |
Cefacetrile binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. This binding inhibits the transpeptidase activity of PBPs, preventing the cross-linking of peptidoglycan chains, which is essential for bacterial cell wall integrity. This leads to cell lysis and bacterial death. As a first-generation cephalosporin, it is effective against a range of Gram-positive and Gram-negative bacteria.
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| ln Vitro |
Less than 1 μg/mL of cefacetrile inhibits both Streptococcus pyogenes and Staphylococcus aureus [2].
Cefacetrile is a broad-spectrum first-generation cephalosporin antibiotic. It is active against numerous Gram-positive and Gram-negative bacteria, including clinical isolates of S. aureus and S. epidermidis. Its in vitro activity is consistent with its mechanism of inhibiting bacterial cell wall synthesis. |
| ln Vivo |
In term fetuses in rats, ceftriline (50, 100, and 500 mg/kg, subcutaneously) does not affect fertility, pregnancy, or postnatal development; in rabbits, it has no effect on any of these parameters [3]. Rats and rabbits do not experience nephrotoxicity from cephalosporins administered intravenously at a dose of 1 g/kg [4].
Cefacetrile is used to treat certain infections caused by bacteria, including infections of the skin, throat, tonsils, and urinary tract. It is also used for the treatment of mammary infections in lactating cows (as Vetimast). Its in vivo efficacy is established through its clinical use. |
| Enzyme Assay |
Cefacetrile's antibacterial activity is assessed using standard in vitro microbiological susceptibility testing methods. Minimum inhibitory concentration (MIC) determinations are performed against various bacterial strains. The compound's binding affinity to penicillin-binding proteins (PBPs) can be evaluated using competitive binding assays.
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| Cell Assay |
Cellular assays for cefacetrile are conducted using standard microbiological techniques with bacterial cultures. The compound's antibacterial activity is evaluated by determining the minimum inhibitory concentration (MIC) against various bacterial strains. Bacterial growth inhibition is assessed by measuring optical density or by counting colony-forming units.
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| Animal Protocol |
In vivo animal model protocols for cefacetrile would involve its administration to animal models of infection to evaluate its efficacy. Studies may include models of skin, throat, tonsil, and urinary tract infections. The compound's efficacy in treating mammary infections in cows has been established in veterinary practice.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Volume of Distribution (Vd): 0.2 to 0.5 L/kg/hour Biological Half-Life: 1.2 hours Cefacetrile has a molecular weight of 339.32 and a molecular formula of C13H13N3O6S. It is a first-generation cephalosporin administered parenterally. Specific pharmacokinetic data is not extensively detailed in the available literature. |
| Toxicity/Toxicokinetics |
Protein Binding
23% to 38% Cefacetrile is generally well-tolerated as a cephalosporin antibiotic. Common adverse effects associated with cephalosporins include gastrointestinal disturbances, hypersensitivity reactions (particularly in patients with penicillin allergy), and local reactions at the injection site. |
| References | |
| Additional Infomation |
Cefacetrile is a cephalosporin antibiotic, a derivative of 7-aminocephalosporin acid. It is a broad-spectrum first-generation cephalosporin with antibacterial activity. It 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 cell wall remodeling 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 bacterial cell walls. This leads to cell wall fragility and subsequent cell lysis.
A derivative of 7-aminocephalosporin acid. Drug Indications Ceftriaxone is a broad-spectrum first-generation cephalosporin antibiotic effective against both Gram-positive and Gram-negative bacteria. Mechanism of Action In vitro studies have shown that the bactericidal effect of cephalosporins stems from their inhibition of cell wall synthesis. Cephalosporins inhibit the third (and final) stage of bacterial cell wall synthesis by binding to specific penicillin-binding proteins (PBPs) located within the bacterial cell wall. Subsequently, bacterial cell wall autolysins (such as autolysins) mediate cell lysis. Cefacetrile (CAS# 10206-21-0) is a broad-spectrum first-generation cephalosporin antibiotic. It is effective against both Gram-positive and Gram-negative bacteria and is used to treat infections of the skin, throat, tonsils, and urinary tract. It is also used in veterinary medicine. |
| Molecular Formula |
C13H13N3O6S
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|---|---|
| Molecular Weight |
339.32
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| Exact Mass |
339.053
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| CAS # |
10206-21-0
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| Related CAS # |
Cefacetrile-13C3
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| PubChem CID |
91562
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.59g/cm3
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| Boiling Point |
757.5ºC at 760mmHg
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| Melting Point |
133-135°C
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| Flash Point |
412ºC
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| Vapour Pressure |
4.02E-25mmHg at 25°C
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| Index of Refraction |
1.639
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| LogP |
-0.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
23
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| Complexity |
664
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(=O)OCC1=C(N2[C@@H]([C@@H](C2=O)NC(=O)CC#N)SC1)C(=O)O
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| InChi Key |
RRYMAQUWDLIUPV-BXKDBHETSA-N
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| InChi Code |
InChI=1S/C13H13N3O6S/c1-6(17)22-4-7-5-23-12-9(15-8(18)2-3-14)11(19)16(12)10(7)13(20)21/h9,12H,2,4-5H2,1H3,(H,15,18)(H,20,21)/t9-,12-/m1/s1
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| Chemical Name |
(6R,7R)-3-(acetyloxymethyl)-7-[(2-cyanoacetyl)amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
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| Synonyms |
Cefacetril; Cephacetrile; Cefacetrile
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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 |
| 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 : ~100 mg/mL (~294.71 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9471 mL | 14.7354 mL | 29.4707 mL | |
| 5 mM | 0.5894 mL | 2.9471 mL | 5.8941 mL | |
| 10 mM | 0.2947 mL | 1.4735 mL | 2.9471 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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