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Ceftaroline FosaMil Inner salt

Names

[ CAS No. ]:
229016-73-3

[ Name ]:
Ceftaroline FosaMil Inner salt

[Synonym ]:
(6R,7R)-7-[[(2E)-2-ethoxyimino-2-[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetyl]amino]-3-[[4-(1-methylpyridin-1-ium-4-yl)-1,3-thiazol-2-yl]sulfanyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
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-,inner salt
Ceftaroline FosaMil Inner salt

Biological Activity

[Description]:

Ceftaroline fosamil (TAK-599) inner salt, a cephalosporin derivative, is an N-phosphono prodrug of anti-methicillin-resistant Staphylococcus aureus (MRSA) T-91825. Ceftaroline fosamil inner salt can be used for the research of MRSA infection[1][2][3].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Bacterial

[In Vivo]

Ceftaroline fosamil inner salt (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 inner salt (10 mg/kg; s.c.) disappeares rapidly and converts smoothly into T-91825 in blood of rats and monkeys[1].

[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.

[2]. Jacqueline C, et, al. In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model. Antimicrob Agents Chemother. 2007 Sep;51(9):3397-400.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H22N8O8PS4

[ Molecular Weight ]:
685.69300

[ Exact Mass ]:
685.01800

[ PSA ]:
344.02000

[ LogP ]:
1.41980

Related Compounds