Fosfomycin tromethamine(Synonyms: 磷霉素氨丁三醇; MK-0955 tromethamine)

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Fosfomycin tromethamine (Synonyms: 磷霉素氨丁三醇; MK-0955 tromethamine)

Fosfomycin (MK-0955) tromethamine 是一种能透过血脑屏障的广谱抗生素，不可逆地抑制细胞壁合成的早期阶段。Fosfomycin tromethamine 对多种细菌具有杀菌活性，这些细菌包括耐多药 (MDR)，广泛耐药 (XDR) 和耐全药 (PDR) 细菌。

Fosfomycin tromethamine(Synonyms: 磷霉素氨丁三醇; MK-0955 tromethamine)

Fosfomycin tromethamine Chemical Structure

CAS No. : 78964-85-9

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Fosfomycin tromethamine 的其他形式现货产品:

Fosfomycin calcium Fosfomycin sodium

生物活性

Fosfomycin (MK-0955) tromethamine is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[1][2].

体外研究
(In Vitro)

Fosfomycin tromethamine is an epoxy antibacterial agent. Compared with other antibacterial agents, it acts by inhibiting the early process of cell wall synthesis[1].
Fosfomycin tromethamine has bactericidal activity against a variety of gram-negative and gram-positive pathogens, including broad-spectrum production β-Bacteria of lactamase and carbapenemase, and against S. aureus strains with an inhibition rate of 90%[1].
Fosfomycin tromethamine displays extensive tissue penetration, can be used to research of infections of the CNS, soft tissues, bone, lungs, and abscesses[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Fosfomycin tromethamine (80 mg/kg; i.v.-i.v. or i.v.-p.o.) displays the protective effect on the nephrotoxicity of double beckacin, and is not affected by different administration routes in rats[3].
Pharmacokinetic of Fosfomycin Tromethamine in Rats[4]

Dibekacin Dose (mg) Vdss (l/kg) β (min-1) T1/2 (min) Urinary recovery (%)
30 0.261 0.0244 28.4 85

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Fischer 344 rats[3]
Dosage: 320 mg/kg
Administration: Intramuscular injection, 5 schedules: 1 h, 0.5 h earlier than dibekacin, concomitantly, 0.5 h later and 1 h later; 11 days
Result: Reduced polyuria, proteinuria, enzymes and cytosine caused by dibecacin (40 mg/kg), followed by the previous treatment.
Animal Model: Dehydrated Wistar rat with acute renal failure (8-week-old)[4]
Dosage: 120 mg/kg
Administration: Intravenous injection; once
Result: Recovered the exclusion rate of rats basically to normal, and improved the nephrotoxicity parameters.
Protects proximal tubular lysosomes from aminoglycosides by inhibiting myeloid formation and protecting the integrity of lysosomal membrane of rats treated with double bekacin.

Clinical Trial

分子量

259.19

Formula

C7H18NO7P
CAS 号

78964-85-9
中文名称

磷霉素氨丁三醇
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Dijkmans AC, et al. Fosfomycin: Pharmacological, Clinical and Future Perspectives. Antibiotics (Basel). 2017 Oct 31;6(4). pii: E24.

    [2]. Falagas ME, et al. Fosfomycin. Clin Microbiol Rev. 2016 Apr. 29(2):321-47.

    [3]. Inouye S, et al. Protective effect of fosfomycin on the experimental nephrotoxicity induced by dibekacin. J Pharmacobiodyn. 1982 Sep. 5(9):659-69.

    [4]. Inouye S, et al. Mode of protective action of fosfomycin against dibekacin-induced nephrotoxicity in the dehydrated rats. J Pharmacobiodyn. 1982 Dec. 5(12):941-50.

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