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CAS No.: 122547-49-3

Faropenem sodium/法罗培南钠 Catalog No. CSN21641

Synonyms: FAROPENEMSODIUMSALTHEMIPENTAHYDRATE;ALP-201;Fropenum sodium

Faropenem sodium is an antibiotic used to treat infections in the ears, nose, throat, urinary tract, skin, and lungs, caused by bacteria.

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技术信息

生物活性

描述Faropenem sodium is a penem antimicrobial that demonstrates a wide antimicrobial spectrum against both aerobic and anaerobic bacteria. It is stable against a number of β-lactamases. E. coli strains were in general susceptible to faropenem, including fluoroquinolone- and cephalosporin-resistant strains^[1]. Faropenem, a stable and orally bioavailable β-lactam, efficiently kills Mycobacterium tuberculosis even in the absence of clavulanate. The target enzymes, L,D-transpeptidases, were inactivated 6- to 22-fold more efficiently by faropenem than by meropenem. Faropenem also showed superior activity against a cryptic subpopulation of nongrowing but metabolically active cells, which may correspond to the viable but nonculturable forms believed to be responsible for relapses following prolonged chemotherapy^[2]. Faropenem was transported via Npt1 with a Michaelis-Menten constant of 0.77 +/- 0.34 mM in a sodium-independent but chloride ion-sensitive manner. When the concentration of chloride ions was increased, the transport activity of faropenem by Npt1 was decreased. The rate of efflux of faropenem from Npt1-expressing oocytes was about 9.5 times faster than that from control water-injected Xenopus oocytes. Zwitterionic beta-lactam antibiotics showed lesser inhibitory effects on faropenem uptake than anionic derivatives, indicating that Npt1 preferentially transports anionic compounds^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02393586	Tuberculosis	Phase 1	Completed	-	Singapore ... more >> National University Hospital Singapore, Singapore Collapse <<

参考文献

[1] Hamasuna R, Tanaka K, Hayami H, et al. Treatment of acute uncomplicated cystitis with faropenem for 3 days versus 7 days: multicentre, randomized, open-label, controlled trial. J Antimicrob Chemother.2014;69(6):1675‐1680
[2] Dhar N, Dubée V, Ballell L, et al. Rapid cytolysis of Mycobacterium tuberculosis by faropenem, an orally bioavailable β-lactam antibiotic. Antimicrob Agents Chemother. 2015;59(2):1308‐1319
[3] Uchino H, Tamai I, Yabuuchi H, et al. Faropenem transport across the renal epithelial luminal membrane via inorganic phosphate transporter Npt1. Antimicrob Agents Chemother. 2000;44(3):574‐577

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2542 mL
- 16.2709 mL
- 32.5417 mL
- 5 mM
- 0.6508 mL
- 3.2542 mL
- 6.5083 mL
- 10 mM
- 0.3254 mL
- 1.6271 mL
- 3.2542 mL

技术信息

CAS号

122547-49-3

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H14NNaO5S

运输

蓝冰

分子量

307.30

别名

FAROPENEMSODIUMSALTHEMIPENTAHYDRATE;ALP-201;Fropenum sodium;SUN-5555;SY-5555;YM-044;法罗培南钠

溶解度

DMSO	315.0 mg/mL (1025.1 mM)
Water	83.0 mg/mL (270.1 mM)

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