CAS NO: | 80210-62-4 |
包装 | 价格(元) |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
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 | ≤10mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in methanol;5mg/ml in acetonitrile |
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 |
Canonical SMILES | O=C(N1[C@]2([H])SCC(COC)=C1C(O)=O)[C@H]2NC(/C(C3=CSC(N)=N3)=N\OC)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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.
细胞实验 [1]: | |
细胞系 | 肺炎链球菌 |
溶解方法 | 在DMSO中的溶解度≤10mg/ml。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应时间 | 23.5mg/kg |
应用 | CS-834对由青霉素敏感性肺炎链球菌引起的肺炎的治疗效果优于头孢地尼,与头孢特仑酯和头孢妥仑酯相当,但不如cefpodoxime proxetil。然而,CS-834对由青霉素耐药的肺炎链球菌引起的肺炎表现出最强的治疗效果。 |
动物实验 [1]: | |
动物模型 | 雄性ddY小鼠 |
剂量 | 口服0.2 mL 0.5%羧甲基纤维素钠盐 |
应用 | 七天后,口服cefpodoxime的小鼠具有良好的抗链球菌和肺炎克雷伯菌感染的能力。 |
注意事项 | 请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。 |
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. |