| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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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].
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| 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].
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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 following intramuscular injection. Bioavailability is 60% following intramuscular injection. Biological Half-Life Approximately 1 hour. |
| Toxicity/Toxicokinetics |
Protein Binding
40% |
| 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 |
Cefotiam is a cephalosporin with ({1-[2-(dimethylamino)ethyl]-1H-tetrazol-5-yl}sulfanyl)methyl and (2-amino-1,3-thiazol-4-yl)acetamido substituents at positions 3 and 7, respectively, of the cephem skeleton. A third generation beta-lactam cephalosporin antibiotic, it is active against a broad spectrum of both Gram positive and Gram negative bacteria. It has a role as an antibacterial drug. It is a cephalosporin, a semisynthetic derivative and a beta-lactam antibiotic allergen.
One of the cephalosporins that has a broad spectrum of activity against both gram-positive and gram-negative microorganisms. Cefotiam has been reported in Bos taurus with data available. Cefotiam is a third-generation, semi-synthetic, beta-lactam cephalosporin antibiotic with antibacterial activity. Cefotiam binds to penicillin-binding proteins (PBPs), transpeptidases that are responsible for crosslinking of peptidoglycan. By preventing crosslinking of peptidoglycan, cell wall integrity is lost and cell wall synthesis is halted. One of the CEPHALOSPORINS that has a broad spectrum of activity against both gram-positive and gram-negative microorganisms. Drug Indication For treatment of severe infections caused by susceptible bacteria. Mechanism of Action The bactericidal activity of cefotiam results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). Pharmacodynamics Cefotiam is a third generation beta-lactam cephalosporin antibiotic that works by inhibiting bacterial cell wall biosynthesis. It is a broad spectrum antibiotic that is effective against Gram positive and Gram negative bacteria. |
| Molecular Formula |
C18H24CLN9O4S3
|
|---|---|
| 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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