| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Cefotiam Hydrochloride targets bacterial cell wall synthesis. It inhibits the transpeptidase enzyme (penicillin-binding proteins, PBPs) that cross-links peptidoglycan chains, a critical component of the bacterial cell wall. By binding to PBPs, it disrupts cell wall synthesis, leading to cell lysis and death. Cefotiam has a broader spectrum of activity compared to first-generation cephalosporins.
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| ln Vitro |
Cefotiam hydrochloride (SCE-963; 0-6.25 μg/mL; 8 h) has antibacterial activity against P. mirabilis IFO 3849, with a minimum inhibitory concentration (MIC) of 1.56 μg/mL [1]. Highly effective against Staphylococcus aureus and Staphylococcus aureus is cefotiam (SCE-963; 0-6.25 μg/mL; 8 h) hydrochloride. Both Staphylococcus aureus (27 strains, MIC values 0.5–1 μg/mL) and Staphylococcus aureus. albus (8 strains, MIC 0.25–0.5 μg/mL) are present. All 29 hemolytic streptococcus strains, 9 pneumococci strains, and 6 viridans streptococci strains had minimum inhibitory concentrations (MICs) between 0.06-4 μg/mL [2].
In vitro, Cefotiam Hydrochloride demonstrates bactericidal activity against a wide range of gram-positive and gram-negative bacteria, including Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, Klebsiella pneumoniae, and Haemophilus influenzae. Its antibacterial activity is characterized by MIC values against susceptible organisms. |
| ln Vivo |
Mice with urinary tract infections caused by Proteus mirabilis can be treated with cefotiam hydrochloride (SCE-963; 12.5-800 mg/kg; intravenously; twice daily for 5 days), which reduces or eradicates the bacterium in the kidneys and bladder wall [1].
Cefotiam Hydrochloride is administered via intravenous or intramuscular injection. It is used for the treatment of respiratory tract infections, urinary tract infections, skin and soft tissue infections, and other bacterial infections. The compound achieves therapeutic concentrations in various tissues and body fluids. |
| Enzyme Assay |
The antibacterial activity of Cefotiam Hydrochloride is assessed using standard antimicrobial susceptibility testing methods, such as broth microdilution or agar diffusion assays. The MIC against various bacterial strains is determined by incubating bacteria with serial dilutions of the compound and observing growth inhibition.
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| Animal Protocol |
Animal/Disease Models: Kiwi fruit xenograft in female CF1/b mice [1] Doses: 12.5, 25, 50, 100, 200, 400 and 800 mg/kg twice (two times) daily for 5 days
Experimental Results: The day after the end of treatment The mice that were sacrificed had diminished or complete eradication of bacteria in their bladder walls and kidneys. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Rapidly absorbed after intramuscular injection. Bioavailability after intramuscular injection is 60%. Biological Half-Life Approximately 1 hour. Cefotiam Hydrochloride has a molecular formula of C18H24ClN9O4S3 and a molecular weight of 562.08 g/mol. Its CAS number is 66309-69-1. It is a white to off-white crystalline powder. It is soluble in water. It should be stored according to the manufacturer's instructions. |
| Toxicity/Toxicokinetics |
Protein Binding
40% Cefotiam Hydrochloride is generally well-tolerated. Common side effects include pain at the injection site, gastrointestinal disturbances, and allergic reactions. It is contraindicated in patients with a history of hypersensitivity to cephalosporins or penicillins. As with all antibiotics, it should be used under medical supervision. |
| References |
[1]. Iwahi T, et, al. Comparative activities of cefotiam and cefazolin against urinary tract infections with Proteus mirabilis in mice. Antimicrob Agents Chemother. 1980 Aug;18(2):257-63.
[2]. Watt B, et, al. In-vitro activity of cefotiam against bacteria of clinical interest. J Antimicrob Chemother. 1982 Nov;10(5):391-5. |
| Additional Infomation |
Cefotaxime is a cephalosporin antibiotic with a cephalosporin skeleton containing a ({1-[2-(dimethylamino)ethyl]-1H-tetrazole-5-yl}thio)methyl group and a (2-amino-1,3-thiazol-4-yl)acetamido group substituent at positions 3 and 7, respectively. As a third-generation β-lactam cephalosporin antibiotic, it exhibits broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria. It is an antibacterial drug. It is a cephalosporin antibiotic, a semi-synthetic derivative, and also a β-lactam antibiotic allergen. It is a broad-spectrum cephalosporin with antibacterial activity against both Gram-positive and Gram-negative bacteria. Cefotaxime has been reported to exist in bovine (Bos taurus) animals, and relevant data exist. Cefotaxime is a third-generation semi-synthetic β-lactam cephalosporin antibiotic with antibacterial activity. Cefotaxime binds to penicillin-binding proteins (PBPs), which are peptidase transpeptidases responsible for peptidoglycan cross-linking. By preventing peptidoglycan cross-linking, cell wall integrity is disrupted, and cell wall synthesis ceases. Cefotaxime is a cephalosporin antibiotic with broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria. Indications: Used to treat severe infections caused by susceptible bacteria. Mechanism of Action: The bactericidal activity of cefotaxime derives from its affinity for penicillin-binding proteins (PBPs), thereby inhibiting cell wall synthesis. Pharmacodynamics: Cefotaxime is a third-generation β-lactam cephalosporin antibiotic whose mechanism of action is through the inhibition of bacterial cell wall biosynthesis. It is a broad-spectrum antibiotic effective against both Gram-positive and Gram-negative bacteria.
Cefotiam Hydrochloride is a second-generation cephalosporin antibiotic used for the treatment of various bacterial infections. It inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins. |
| Molecular Formula |
C18H24CLN9O4S3
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|---|---|
| Molecular Weight |
562.0891
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| Exact Mass |
597.056
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| CAS # |
66309-69-1
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| Related CAS # |
Cefotiam hexetil hydrochloride;95789-30-3;Cefotiam;61622-34-2;Cefotiam dihydrochloride hydrate
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| PubChem CID |
43708
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| Appearance |
White to off-white solid powder
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| Boiling Point |
940ºC at 760 mmHg
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| LogP |
1.058
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
848
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| Defined Atom Stereocenter Count |
2
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| SMILES |
Cl[H].S1C([H])([H])C(C([H])([H])SC2=NN=NN2C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])=C(C(=O)O[H])N2C([C@]([H])([C@@]12[H])N([H])C(C([H])([H])C1=C([H])SC(N([H])[H])=N1)=O)=O
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| InChi Key |
QYQDKDWGWDOFFU-IUODEOHRSA-N
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| InChi Code |
InChI=1S/C18H23N9O4S3/c1-25(2)3-4-26-18(22-23-24-26)34-7-9-6-32-15-12(14(29)27(15)13(9)16(30)31)21-11(28)5-10-8-33-17(19)20-10/h8,12,15H,3-7H2,1-2H3,(H2,19,20)(H,21,28)(H,30,31)/t12-,15-/m1/s1
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| Chemical Name |
(6R,7R)-7-[[2-(2-amino-1,3-thiazol-4-yl)acetyl]amino]-3-[[1-[2-(dimethylamino)ethyl]tetrazol-5-yl]sulfanylmethyl]-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: (1). This product is not stable in solution, please use freshly prepared working solution for optimal results. (2). 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 : ~100 mg/mL (~167.07 mM)
H2O : ~33.33 mg/mL (~55.68 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.18 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 25.0 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: ≥ 2.5 mg/mL (4.18 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 25.0 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: ≥ 2.5 mg/mL (4.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (83.54 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 | 1.7791 mL | 8.8954 mL | 17.7907 mL | |
| 5 mM | 0.3558 mL | 1.7791 mL | 3.5581 mL | |
| 10 mM | 0.1779 mL | 0.8895 mL | 1.7791 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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