β-lactam

At least 90% of the strains tested (MIC90) for the Enterobacteriaceae ranged from 0.06 to 8 μg/mL when cefmenoxime (SCE-1365) hydrochloride was used[1].
The MIC90 values for gram-positive cocci that are inhibited by cefmenoxime (SCE-1365) hydrochloride are 2 μg/mL for S. aureus and 0.015 and ≤0.008 μg/mL for Streptococcus pneumoniae and Streptococcus pyogenes, respectively[1].
With MIC90 values ranging from ≤0.008 to 0.25 μg/mL, cefmenoxime (SCE-1365) hydrochloride is effective against Haemophilus influenzae, Neisseria gonorrhoeae, and Neisseria meningitidis[1].

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Cefmenoxime exhibited broad-spectrum antimicrobial activity against 486 clinical isolates. Its activity was compared with cefazolin, cefoxitin, cefamandole (all 486 isolates), and cefotaxime (114 isolates). Against Enterobacteriaceae, the MIC₉₀ ranged from 0.12 μg/ml (Escherichia coli) to 8 μg/ml (Serratia marcescens). For gram-positive cocci, MIC₉₀ was ≤0.008 μg/ml for Streptococcus pyogenes, 0.015 μg/ml for Streptococcus pneumoniae, and 2 μg/ml for Staphylococcus aureus. Group D streptococci were less susceptible (MIC₉₀ = 16 μg/ml). Cefmenoxime was very active against Haemophilus influenzae (MIC₉₀ ≤0.008 μg/ml), Neisseria gonorrhoeae (MIC₉₀ = 0.015 μg/ml), and Neisseria meningitidis (MIC₉₀ = 0.25 μg/ml). Against Pseudomonas aeruginosa and Acinetobacter spp., 16 μg/ml inhibited 78% and 73% of strains, respectively, with MIC₉₀ values of 32 μg/ml for both. For anaerobes, MICs ranged from 0.5 to >128 μg/ml, with good activity against gram-positive anaerobes but weaker activity against Bacteroides fragilis. [1]
The antibacterial activity of cefmenoxime was primarily bactericidal. For 87% of 31 gram-negative organisms tested, the minimal bactericidal concentration was the same as or only twofold higher than the MIC. [1]
The activity of cefmenoxime was only slightly affected by inoculum size. Increasing the inoculum from 10⁵ to 10⁷ CFU/ml resulted in MIC increases of fourfold or less for 80% of organisms tested. [1]
In synergy studies using the checkerboard technique, the combination of cefmenoxime and gentamicin was synergistic (Fractional Inhibitory Concentration index <0.6) against 80% (8 of 10) of Enterobacteriaceae strains and 100% (9 of 9) of P. aeruginosa strains tested. In the most effective combinations, cefmenoxime concentrations ranged from 0.001 to 0.25 μg/ml for Enterobacteriaceae and 0.5 to 32 μg/ml for P. aeruginosa. [1]
Development of resistance to cefmenoxime in vitro occurred slowly or not at all for E. coli, Klebsiella pneumoniae, Proteus mirabilis, and S. aureus after 14 serial transfers in broth. Resistance developed rapidly for S. marcescens (MIC >512 μg/ml after 2 transfers) and P. aeruginosa (MIC >512 μg/ml after 6 transfers). The development profile was similar to that of cefotaxime. [1]

Mice infected with lung bacteria are more likely to survive when cefmenoxime (SCE-1365) hydrochloride (40 mg/kg; intraperitoneally; daily, for 7 days; male Jcl:ICR mice) is administered.[2]

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The protective efficacy of cefmenoxime was evaluated in a mouse systemic infection model. Female Swiss albino mice were infected intraperitoneally with approximately 100 times the LD₅₀ of various bacteria. Subcutaneous administration of cefmenoxime at 1 and 6 hours post-infection demonstrated protective activity. The PD₅₀ (protective dose for 50% of mice) values for cefmenoxime against different organisms were: E. coli (Juhl): 0.5 mg/kg; Enterobacter cloacae: 0.4-0.5 mg/kg; P. mirabilis: 4.1 mg/kg; Proteus vulgaris: 0.4 mg/kg; P. aeruginosa: 54-127 mg/kg; S. aureus (Smith): 4.1 mg/kg. The protective effect of cefmenoxime was superior to that of cefazolin for all infections except S. aureus. [1]

Animal Model: Male Jcl:ICR mice[2]
Dosage: 40 mg/kg
Administration: Subcutaneous injection; daily, for 7 days
Result: Inhibited mortality rate of animals was 60% at a dose of 40 mg/kg.

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In vivo efficacy was tested in a mouse systemic infection model. Female Swiss albino mice weighing 18-20 g were infected intraperitoneally with a bacterial suspension containing approximately 100 times the LD₅₀ number of organisms in brain heart infusion broth containing 5% aqueous hog gastric mucin. Serial twofold dilutions of cefmenoxime (hemihydrochloride salt) were prepared fresh daily. The drug was administered subcutaneously to groups of 10 mice at 1 and 6 hours post-infection. Mortality was recorded over 7 days. The PD₅₀ and 95% confidence limits were calculated by the trimmed Spearman-Karber method. [1]

[1]. Antimicrobial activity of cefmenoxime (SCE-1365). Antimicrob Agents Chemother. 1981 Mar;19(3):454-60.

[2]. Synergistic effects of romurtide and cefmenoxime against experimental Klebsiella pneumonia in mice. Antimicrob Agents Chemother. 1992 Jan;36(1):167-71.

[3]. Jpn J Antibiot. 1995 May;48(5):602-9..

Cefominoxime hydrochloride is the hydrochloride form of cefominoxime, a third-generation semi-synthetic β-lactam cephalosporin antibiotic with antibacterial activity. Cefominoxime binds to penicillin-binding proteins (PBPs), which are peptidases responsible for the cross-linking of peptidoglycan. By preventing peptidoglycan cross-linking, cell wall integrity is disrupted, and cell wall synthesis ceases. Cefominoxime is a cephalosporin antibiotic that can be administered intravenously or intramuscularly. It is effective against most common Gram-positive and Gram-negative bacteria, is a potent inhibitor of Enterobacteriaceae, and is highly resistant to β-lactamase hydrolysis. This drug has high efficacy against a variety of infections, and no serious side effects have been reported to date. Cefominoxime (proposed international nonproprietary name, also known as SCE-1365 or A-50912) is a novel semi-synthetic cephalosporin antibiotic. Its chemical name is 7-β-[2-(2-aminothiazol-4-yl)-(Z)-2-methoxyaminoacetamido]-3-[(1-methyl-1H-tetrazol-5-yl)thioethyl]cefo-3-em-4-carboxylic acid hemihydrochloride. [1]
Its potent broad-spectrum antibacterial activity, bactericidal effect, slow development of in vitro resistance, minimal inoculation effect, and protective efficacy demonstrated in mice make it a potential effective therapeutic drug. [1]
In vitro experiments have shown that cefominoxetine combined with gentamicin has synergistic activity against most Enterobacteriaceae and Pseudomonas aeruginosa strains. [1]

C32H35CLN18O10S6

1059.5779

1058.079

C, 36.27; H, 3.33; Cl, 3.35; N, 23.80; O, 15.10; S, 18.15

75738-58-8

Cefmenoxime;65085-01-0

11954009

Solid powder

0.04

7

28

16

67

890

4

Cl[H].S1C([H])([H])C(C([H])([H])SC2=NN=NN2C([H])([H])[H])=C(C(=O)O[H])N2C([C@]([H])([C@@]12[H])N([H])C(/C(/C1=C([H])SC(N([H])[H])=N1)=N\OC([H])([H])[H])=O)=O.S1C([H])([H])C(C([H])([H])SC2=NN=NN2C([H])([H])[H])=C(C(=O)O[H])N2C([C@]([H])([C@@]12[H])N([H])C(/C(/C1=C([H])SC(N([H])[H])=N1)=N\OC([H])([H])[H])=O)=O

MPTNDTIREFCQLK-RGZOMKIGSA-N

InChI=1S/2C16H17N9O5S3.ClH/c2*1-24-16(20-22-23-24)33-4-6-3-31-13-9(12(27)25(13)10(6)14(28)29)19-11(26)8(21-30-2)7-5-32-15(17)18-7;/h2*5,9,13H,3-4H2,1-2H3,(H2,17,18)(H,19,26)(H,28,29);1H/b2*21-8+;

7-[[(2E)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-[(1-methyltetrazol-5-yl)sulfanylmethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid;hydrochloride

Cefmenoxime Hydrochloride; SCE 1365 hydrochloride; AB 50912 hemihydrochloride; EINECS 278-299-4; SCE1365; Hydrochloride, Cefmenoxime; SCE 1365; SCE-1365;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~65 mg/mL (~122.69 mM) H2O : < 0.1 mg/mL

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)