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- Cefpodoxime (free acid)
Cefpodoxime (free acid)
Cefpodoxime, as known as R 3763, is a metabolite of cefpodoxime proxetil. It is demonstrated that cefpodoxime, as an oral third generation cephalosporin antibiotic, is active against most Gram-positive and Gram-negative bacteria.
Cefpodoxime suppresses bacterial septum and cell wall synthesis by binding to penicillin-binding proteins (PBPs) located in the bacterial cytoplasmic membrane.
In vitro: Cefpodoxime showed antibacterial activities against obligatory anaerobes and salmonella spp., shigella spp. and Neisseria meningitides. The activity of cefpodoxime was less active than R95867, an active form of CS-834, against Gram-negative bacteria [1]. Cefpodoxime was quite stable to hydrolysis by β-lactamases produced from B. cereus and E. coli HB101/pBR322 [2].
In vivo: Male ddY mice were administered orally in a volume of 0.2 mL of 0.5% carboxymethyl cellulose sodium salt. After 7 days, it was shown that cefpodoxime had good efficacy against streptococcus spp. and K. pneumoniae infection in mice [1].
References:
[1].? Sakagawa, E., Otsuki, M., Oh, T., & Nishino, T. In-vitro and in-vivo antibacterial activities of CS-834, a new oral carbapenem. Journal of Antimicrobial Chemotherapy, 1998; 42: 426-437.
[2].? Fukuoka, T., Ohya, S., Utsui, Y., Domon, H., Takenouchi, T., Koga, T., … Kuwahara, S. In vitro and in vivo antibacterial activities of CS-834, a novel oral carbapenem. Antimicrobial Agents and Chemotherapy, 1997; 41(12): 2652–2663.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 427.5 |
Cas No. | 80210-62-4 |
Formula | C15H17N5O6S2 |
Synonyms | R 3763 |
Solubility | ≥50 mg/mL in DMSO |
Chemical Name | (6R)-7R-[[(2Z)-2-(2-amino-4-thiazolyl)-2-(methoxyimino)acetyl]amino]-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid |
SDF | Download SDF |
Canonical SMILES | O=C(N1[C@]2([H])SCC(COC)=C1C(O)=O)[C@H]2NC(/C(C3=CSC(N)=N3)=N\OC)=O |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment [1]: | |
Cell lines |
S. pneumoniae. |
Preparation method |
The solubility of this compound in DMSO is ≤10mg/ml in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
23.5mg/kg |
Applications |
CS-834 is superior to cefdinir in the treatment of pneumonia caused by penicillin-sensitive Streptococcus pneumoniae, and is comparable to cefpodoxime and cefpodoxime, but not as good as cefpodoxime proxetil. However, CS-834 shows the strongest therapeutic effect on pneumonia caused by penicillin-resistant Streptococcus pneumoniae. |
Animal experiment [1]: | |
Animal models |
Male ddY mice |
Dosage form |
Administered orally in a volume of 0.2 mL of 0.5% carboxymethyl cellulose sodium salt |
Application |
Seven days later, mice that received oral cefpodoxime had good resistance to streptococcus and Klebsiella pneumoniae infections. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Sakagawa E, Otsuki M, Oh T, Nishino T. In-vitro and in-vivo antibacterial activities of CS-834, a new oral carbapenem. J Antimicrob Chemother. 1998 Oct;42(4):427-37. Erratum in: J Antimicrob Chemother 1999 Jan;43(1):169. Ou T [corrected to Oh T]. PubMed PMID: 9818740. |
Quality Control & MSDS
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