| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Cefotiam (SCE-963; 0-6.25 μg/mL; 8 h) shows MIC value of 1.56 μg/mL antibacterial activity against P. mirabilis IFO 3849 [1]. Cefotiam exhibits excellent activity against Staphylococcus aureus and Staphylococcus aureus (0–6.25μg/mL; 8 hours). MIC values for Staphylococcus aureus (27 strains) and Staphylococcus aureus. albus (8 strains) range from 0.25 to 0.5 μg/mL. The minimum inhibitory concentration (MIC) ranged from 0.06-4 μg/mL for all 29 strains of hemolytic streptococcus, 9 strains of pneumococci, and 6 strains of viridans streptococci [2].
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|---|---|
| ln Vivo |
Mice with urinary tract infections caused by Proteus mirabilis can be cured of these infections by administering cefotiam (SCE-963; 12.5-800 mg/kg; intravenously; twice daily for five days) which also reduces or eliminates bacteria in the kidneys and bladder wall [1].
|
| 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. |
| 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 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. Cefotiam has been reported to exist in bovine (Bos taurus) animals, and relevant data exist. Cefotiam is a third-generation semi-synthetic β-lactam cephalosporin antibiotic with antibacterial activity. Cefotiam 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. Cefotiam 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 Cefotiam derives from its affinity for penicillin-binding proteins (PBPs), thereby inhibiting cell wall synthesis. Pharmacodynamics: Cefotiam 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.
|
| Molecular Formula |
C18H23N9O4S3
|
|---|---|
| Molecular Weight |
525.63
|
| Exact Mass |
525.103
|
| CAS # |
61622-34-2
|
| Related CAS # |
Cefotiam hydrochloride;66309-69-1;Cefotiam dihydrochloride hydrate
|
| PubChem CID |
43708
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.8±0.1 g/cm3
|
| Index of Refraction |
1.855
|
| LogP |
0.24
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
13
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
34
|
| Complexity |
848
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
O=C(C(N12)=C(CSC3=NN=NN3CCN(C)C)CS[C@]2([H])[C@H](NC(CC4=CSC(N)=N4)=O)C1=O)O
|
| InChi Key |
QYQDKDWGWDOFFU-IUODEOHRSA-N
|
| 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
|
| 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
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 1.9025 mL | 9.5124 mL | 19.0248 mL | |
| 5 mM | 0.3805 mL | 1.9025 mL | 3.8050 mL | |
| 10 mM | 0.1902 mL | 0.9512 mL | 1.9025 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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