| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Cefathiamidine targets bacterial cell wall synthesis. As a cephalosporin antibiotic, it inhibits penicillin-binding proteins (PBPs), which are essential for bacterial cell wall peptidoglycan synthesis. By binding to PBPs, it disrupts cell wall formation, leading to bacterial cell lysis and death. Its activity is bactericidal.
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| ln Vitro |
The study examined and contrasted cefathiamidine's in vitro efficacy against Streptococcus faecalis and Streptococcus faecium with that of other β-lactam medications. Each of the 56 Str strains. The Enterococcus faecalis test was suppressed by cefthiamidin at a dose of 2 mg/L. Ampicillin with cefthiamidine against ten different Streptococcus bacteria' MBCs. Streptococcus faecalis has an MBC/MIC ratio more than 64. A higher concentration of ampicillin and cefathiamidine than the minimum inhibitory concentration (MIC) reduces enterococci faecalis. Ampicillin 4 mg/L or cefthiamidin 2 mg/L are the most rapid killers. This paradoxical bactericidal action was removed when adding 1 mg/L of gentamicin. According to time-disinfect tests, beta-lactams and aminoglycosides together kill 99.9% of cells in 6 hours [2].
Cefathiamidine exhibits a wide spectrum of antimicrobial activity against Gram-positive bacteria. It is particularly active against Staphylococcus aureus, Viridans streptococci, and Streptococcus pneumoniae. It shows unique antibacterial activity against Enterococcus. It also has activity against some Gram-negative bacteria. |
| ln Vivo |
Cefathiamidine is given parenterally, meaning it is injected intravenously or intramuscularly, as it is not absorbed orally. While ceftizamidine is extensively dispersed across the majority of bodily fluids and tissues, cefothioamidine is unable to pass through the blood-brain barrier. Cefathiamidine has a 23% protein binding capability, and the kidneys eliminate more than 90% of it unaltered [1].
Cefathiamidine is used to treat infections caused by susceptible bacteria, including respiratory tract infections, biliary tract infections, urinary tract infections, gynecological infections, sepsis, pneumonia, and meningitis. It is administered by intramuscular or intravenous injection. Its efficacy has been demonstrated in clinical practice, particularly in China where it was first developed. |
| Enzyme Assay |
In vitro assays for Cefathiamidine typically involve antimicrobial susceptibility testing using standardized methods such as broth microdilution or agar dilution. Various bacterial strains are cultured and exposed to serial dilutions of the compound. Minimum inhibitory concentrations (MIC) are determined as the lowest concentration that inhibits visible bacterial growth. The compound's activity is compared to other cephalosporins and antibiotics.
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| Cell Assay |
For in vitro cell-based assays, bacterial cultures are treated with Cefathiamidine at various concentrations. Bacterial growth is monitored by measuring optical density at 600 nm. Time-kill curves can be generated to assess the bactericidal activity. The compound's effects on bacterial cell morphology can be examined by electron microscopy. Cytotoxicity in mammalian cells can be assessed using MTT or other standard assays.
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| Animal Protocol |
In vivo animal studies with Cefathiamidine are conducted in models of bacterial infection. Animals are infected with pathogenic bacteria and treated with the compound via intramuscular or intravenous injection. Efficacy is measured by survival rates, bacterial clearance from tissues, and resolution of infection symptoms. Pharmacokinetic studies assess the compound's distribution, metabolism, and excretion.
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| ADME/Pharmacokinetics |
Cefathiamidine (CAS: 33075-00-2) has a molecular weight of 472.58 g/mol and a molecular formula of C19H28N4O6S2. It is a water-soluble, semi-synthetic cephalosporin antibiotic. Chemical name: (6R,7R)-3-(Acetoxymethyl)-7-(2-(((E)-N,N'-diisopropylcarbamimidoyl)thio)acetamido)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid. Storage: cool, dry place.
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| Toxicity/Toxicokinetics |
Cefathiamidine is a first-generation cephalosporin antibiotic with an established safety profile. Common side effects include allergic reactions (rash, urticaria), gastrointestinal disturbances, and injection site reactions. As with other cephalosporins, cross-hypersensitivity with penicillins may occur. It is contraindicated in patients with a history of hypersensitivity to cephalosporins. It is an approved antibiotic in some countries.
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| References |
[1]. Zhi LJ, et al. Population pharmacokinetics and dosing optimization of cefathiamidine in children with hematologic infection. Drug Des Devel Ther. 2018 Apr 17;12:855-862.
[2]. Chen HY, et al. The killing effects of cefathiamidine or ampicillin alone and in combination with gentamicin against enterococci. J Antimicrob Chemother. 1983 Jul;12(1):19-26. |
| Additional Infomation |
Cefotiam is a cephalosporin.
Cefathiamidine is a first-generation, water-soluble, semi-synthetic cephalosporin antibiotic. It exhibits broad-spectrum bactericidal activity against Gram-positive bacteria, especially Staphylococcus aureus, Viridans streptococci, and Streptococcus pneumoniae, and some Gram-negative bacteria. It was first developed for clinical use in China. It is an approved antibiotic in some countries. |
| Molecular Formula |
C19H28N4O6S2
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|---|---|
| Molecular Weight |
472.57882
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| Exact Mass |
472.145
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| CAS # |
33075-00-2
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| PubChem CID |
15942748
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.653
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| LogP |
2.67
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
31
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| Complexity |
811
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C(C(N12)=C(COC(C)=O)CS[C@]2([H])[C@H](NC(CS/C(NC(C)C)=N/C(C)C)=O)C1=O)O
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| InChi Key |
JYXACOFERDBGGQ-RHSMWYFYSA-N
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| InChi Code |
InChI=1S/C19H28N4O6S2/c1-9(2)20-19(21-10(3)4)31-8-13(25)22-14-16(26)23-15(18(27)28)12(6-29-11(5)24)7-30-17(14)23/h9-10,14,17H,6-8H2,1-5H3,(H,20,21)(H,22,25)(H,27,28)/t14-,17-/m1/s1
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| Chemical Name |
(6R,7R)-3-(acetyloxymethyl)-7-[[2-[N,N'-di(propan-2-yl)carbamimidoyl]sulfanylacetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic 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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~264.51 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.40 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 (4.40 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1160 mL | 10.5802 mL | 21.1604 mL | |
| 5 mM | 0.4232 mL | 2.1160 mL | 4.2321 mL | |
| 10 mM | 0.2116 mL | 1.0580 mL | 2.1160 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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