Basic information Safety Supplier Related

ceftaroline fosamil acetate monohydrate

Basic information Safety Supplier Related

ceftaroline fosamil acetate monohydrate Basic information

Product Name:
ceftaroline fosamil acetate monohydrate
Synonyms:
  • 4-[2-[[(6R,7R)-2-Carboxy-7-[[(2Z)-(ethoxyimino)[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]thio]-4-thiazolyl]-1-methylpyridinium acetate hydrate
  • TAK 599 acetate H2O
  • 4-[2-[[(6R,7R)-2-carboxy-7-[[(2Z)-(ethoxyimino)[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]thio]-4-thiazolyl]-1-methylpyridinium acetate hydra
  • ceftaroline fosamil acetate monohydrate
  • Ceftaroline fosamil (hydrate)(acetate)
  • Pyridinium, 4-[2-[[(6R,7R)-2-carboxy-7-[[(2Z)-2-(ethoxyimino)-2-[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]thio]-4-thiazolyl]-1-methyl-, acetate, hydrate (1:1:1)
  • Ceftaroline fosamil acetate hydrate - Bio-X ?
CAS:
400827-55-6
MF:
C22H22N8O8PS4.C2H3O2.H2O
MW:
762.76
Mol File:
400827-55-6.mol
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ceftaroline fosamil acetate monohydrate Usage And Synthesis

Uses

Ceftaroline fosamil hydrate is a potent cephalosporin antibiotic. Ceftaroline fosamil hydrateshows broad-spectrum activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Streptococcus pneumoniae, and common Gram-negative organisms. Ceftaroline fosamil hydrate has anti-infective activity, and can be used for the research of complicated skin and skin structure infections (cSSSIs) and community-acquired bacterial pneumonia (CABP)[1][2][3].

in vivo

Ceftaroline fosamil hydrate(s.c.) shows protective effects against experimental systemic infection caused by S. aureus N133 in mice, with ED50s of 1.60-2.37 mg/kg[1].
Ceftaroline fosamil hydrate (10 mg/kg; s.c.) disappeares rapidly and converts smoothly into T-91825 in blood of rats and monkeys[1].

IC 50

β-lactam

References

[1] Ishikawa T, et, al. TAK-599, a novel N-phosphono type prodrug of anti-MRSA cephalosporin T-91825: synthesis, physicochemical and pharmacological properties. Bioorg Med Chem. 2003 May 29;11(11):2427-37. DOI:10.1016/s0968-0896(03)00126-3
[2] Biek D, et al. Ceftaroline fosamil: a novel broad-spectrum cephalosporin with expanded anti-Gram-positive activity. J Antimicrob Chemother. 2010 Nov;65 Suppl 4:iv9-16. DOI:10.1093/jac/dkq251
[3] Parish D, et al. Ceftaroline fosamil, a cephalosporin derivative for the potential treatment of MRSA infection. Curr Opin Investig Drugs. 2008 Feb;9(2):201-9. PMID:18246523

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