| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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| Other Sizes |
| Targets |
Cefpodoxime proxetil is a prodrug that is converted to its active form, cefpodoxime, after oral administration. Cefpodoxime exerts its bactericidal activity by binding to penicillin-binding proteins (PBPs), which inhibits peptidoglycan synthesis. This inhibition disrupts bacterial cell wall biosynthesis. Peptidoglycan is the primary constituent of bacterial cell walls, and its inhibition leads to cell lysis and death. Cefpodoxime is stable in the presence of β-lactamase enzymes.
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| ln Vitro |
Cefpodoxime proxetil is a broad-spectrum antibiotic which targets a wide variety of Gram-positive and Gram-negative bacteria, especially those which cause otitis media and pharyngitis. The active form, cefpodoxime, is active against a wide spectrum of Gram-positive and Gram-negative bacteria. It is stable in the presence of β-lactamase enzymes. The compound's broad-spectrum activity makes it effective against a range of clinically significant pathogens.
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| ln Vivo |
Cefpodoxime proxetil is an orally administered prodrug that is absorbed and de-esterified by the intestinal mucosa to release the active third-generation cephalosporin, cefpodoxime. It is used for the treatment of infections caused by susceptible organisms, including otitis media and pharyngitis. The compound's oral bioavailability and broad-spectrum activity make it a valuable option for treating outpatient infections.
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| Enzyme Assay |
Cefpodoxime proxetil's activity is assessed using standard in vitro microbiological susceptibility testing methods. Minimum inhibitory concentration (MIC) determinations are performed against various bacterial strains. The compound's binding affinity to penicillin-binding proteins (PBPs) can be evaluated using competitive binding assays with radiolabeled penicillin. The compound's stability against β-lactamase enzymes can be evaluated using standard β-lactamase inhibition assays.
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| Cell Assay |
Cellular assays for cefpodoxime proxetil are conducted using standard microbiological techniques with bacterial cultures. The compound's antibacterial activity is evaluated by determining the minimum inhibitory concentration (MIC) against various bacterial strains. Bacterial growth inhibition is assessed by measuring optical density or by counting colony-forming units. The compound's activity is evaluated against both Gram-positive and Gram-negative organisms.
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| Animal Protocol |
In vivo animal model experiments for cefpodoxime proxetil would involve oral administration to animal models of infection to evaluate its efficacy. Studies may include models of otitis media, pharyngitis, and other respiratory tract infections. The prodrug is absorbed and de-esterified by the intestinal mucosa to release the active cefpodoxime. Such studies are essential for understanding the compound's in vivo behavior and therapeutic potential.
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| ADME/Pharmacokinetics |
Cefpodoxime proxetil is an orally administered prodrug. It is absorbed and de-esterified by the intestinal mucosa to release the active third-generation cephalosporin, cefpodoxime. Specific pharmacokinetic data is not extensively detailed in the available literature. As an orally active cephalosporin, it is expected to have good oral bioavailability.
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| Toxicity/Toxicokinetics |
Cefpodoxime proxetil is generally well-tolerated as a cephalosporin antibiotic. Common side effects may include gastrointestinal disturbances, allergic reactions, and, in rare cases, superinfection due to disruption of normal flora. Hypersensitivity reactions can occur, particularly in patients allergic to penicillin.
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| References |
Drug Dev Ind Pharm. 2021 Aug;47(8):1261-1278.
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| Additional Infomation |
Cefpodoxime proxetil is a 1-[(isopropoxycarbonyl)oxy]ethyl (ester) prodrug of cefpodoxime. After ingestion, the ester group is hydrolyzed in intestinal epithelial cells, releasing the active ingredient cefpodoxime into the bloodstream. It is used to treat acute otitis media, pharyngitis, and sinusitis. It is both a prodrug and an antibacterial agent. It is a carboxylic acid ester, a cephalosporin antibiotic, and a carboxylic acid antibiotic. Functionally, it is similar to cefpodoxime and 4-{((R)-2-carboxy-3-methoxymethyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-en-7-ylcarbamoyl)-[(Z)-methoxyimino]-methyl}-thiazolyl-2-yl-ammonium salt. Vantin has been reported in the Chinese honeybee (Apis cerana), and relevant data are available. Cefpodoxime proxetil is a third-generation semi-synthetic cephalosporin and a β-lactam antibiotic with bactericidal activity. The action of cefpodoxime depends on its binding to penicillin-binding proteins (PBPs) located on the bacterial cell membrane. This binding inhibits transpeptidase activity, thereby preventing the cross-linking of the pentaglycine bridge to the fourth residue of the pentapeptide and interrupting subsequent peptidoglycan chain synthesis. Therefore, cefpodoxime inhibits the synthesis of bacterial septa and cell walls. Its active metabolite is the prodrug of cefpodoxime. See also: Cefpodoxime (containing the active fraction).
Cefpodoxime Proxetil (CAS# 87239-81-4) is a broad-spectrum antibacterial agent that acts by binding to penicillin-binding proteins (PBPs), thus inhibiting peptidoglycan synthesis. It is an orally administered prodrug that is absorbed and de-esterified by the intestinal mucosa to release the active third-generation cephalosporin, cefpodoxime. It is active against a wide spectrum of Gram-positive and Gram-negative bacteria, especially those which cause otitis media and pharyngitis. |
| Molecular Formula |
C21H27N5O9S2
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|---|---|
| Molecular Weight |
557.6
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| Exact Mass |
557.125
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| Elemental Analysis |
C, 45.23; H, 4.88; N, 12.56; O, 25.82; S, 11.50
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| CAS # |
87239-81-4
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| Related CAS # |
80210-62-4 (free acid);82619-04-3 (sodium);87239-81-4 (Proxetil);79287-88-0 (HCl); 82623-37-8 (TFA);
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| PubChem CID |
6526396
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| Appearance |
White to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Melting Point |
111-113°C
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| Index of Refraction |
1.671
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| LogP |
2.17
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
37
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| Complexity |
976
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C(C1=C(COC)CS[C@@H]2[C@@H](C(N12)=O)NC(=O)/C(/C1=CSC(N)=N1)=N\OC)(=O)OC(C)OC(=O)OC(C)C
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| InChi Key |
LTINZAODLRIQIX-ZFEISNGRSA-N
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| InChi Code |
InChI=1S/C21H27N5O9S2/c1-9(2)33-21(30)35-10(3)34-19(29)15-11(6-31-4)7-36-18-14(17(28)26(15)18)24-16(27)13(25-32-5)12-8-37-20(22)23-12/h8-10,14,18H,6-7H2,1-5H3,(H2,22,23)(H,24,27)/b25-13+/t10?,14-,18-/m1/s1
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| Chemical Name |
1-propan-2-yloxycarbonyloxyethyl (6R,7R)-7-[[(2E)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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| Synonyms |
Banan Vantin Cefpodoxime ProxetilCS-807 Doxef U 76252Doxef CS 807 Toraximcephalosporin 807 CS 807 U-76,252
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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 |
| 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 (~224.18 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.73 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 (3.73 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 (3.73 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 | 1.7934 mL | 8.9670 mL | 17.9340 mL | |
| 5 mM | 0.3587 mL | 1.7934 mL | 3.5868 mL | |
| 10 mM | 0.1793 mL | 0.8967 mL | 1.7934 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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