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Merck

SML2744

Sigma-Aldrich

Sitafloxacin sesquihydrate

≥98% (HPLC)

Sinónimos:

7-[(7S)-7-Amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid, hydrate (2:3), DU 6859 sesquihydrate, DU 6859a sesquihydrate, DU-6859 sesquihydrate, DU-6859a sesquihydrate, DU6859 sesquihydrate, DU6859a sesquihydrate

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About This Item

Fórmula empírica (notación de Hill):
C19H18ClF2N3O3·1.5H2O
Número de CAS:
Peso molecular:
436.84
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77

Nivel de calidad

Análisis

≥98% (HPLC)

formulario

powder

condiciones de almacenamiento

desiccated

color

white to beige

solubilidad

DMSO: 2 mg/mL, clear

temp. de almacenamiento

−20°C

InChI

1S/C19H18ClF2N3O3.H2O/c20-14-15-8(17(26)9(18(27)28)5-25(15)12-4-10(12)21)3-11(22)16(14)24-6-13(23)19(7-24)1-2-19;/h3,5,10,12-13H,1-2,4,6-7,23H2,(H,27,28);1H2/t10-,12+,13+;/m0./s1

Clave InChI

ANCJYRJLOUSQBW-JJZGMWGRSA-N

Acciones bioquímicas o fisiológicas

Sitafloxacin (DU-6859 or DU-6859a) is an orally active, fourth generation fluoroquinolone that exhibits broad-spectrum antibiotic activity against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, via dual inhibitory activity against bacterial DNA gyrase and topoisomerase IV (IC50 = 1.16 and 1.88 μg/mL against S. pneumoniae gyrA/B and parC/E, respectively). Sitafloxacin is active against methicillin-resistant staphylococci, Streptococcus pneumoniae and other streptococci with reduced susceptibility to levofloxacin and other quinolones and enterococci. Sitafloxacin also exhibits activity against clinical isolates of Klebsiella pneumoniae, Enterobacter cloacae, Pseudomonas aeruginosa as well as some activity against quinolone-resistant strains and Acinetobacter baumannii. Sitafloxacin in vitro activity against anaerobes is comparable to imipenem and metronidazole.

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


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Lina Yi et al.
Journal of medical microbiology, 66(6), 770-776 (2017-06-10)
Purpose. Sitafloxacin (SFX) is a new fluoroquinolone (FQ) that has shown a strong bactericidal effect against Mycobacterium tuberculosis (Mtb) in vitro. However, data on SFX efficacy against Mtb with gyrA/B mutations and its epidemiological cut-off (ECOFF) value remain limited. Therefore
Ryoichi Hamasuna et al.
Microbial drug resistance (Larchmont, N.Y.), 24(1), 30-34 (2017-06-06)
Emergence of antimicrobial resistance in Neisseria gonorrhoeae is a major public health concern globally, and new antimicrobials for treatment of gonorrhea are imperative. In this study, the in vitro activity of sitafloxacin, a fluoroquinolone mainly used for respiratory tract or
Xiaomeng Dong et al.
International journal of clinical and experimental medicine, 8(5), 8135-8140 (2015-07-30)
To detect the in vitro activities of sitafloxacin alone and in combination with rifampin, colistin, sulbactam, and tigecycline against extensively drug-resistant Acinetobacter baumannii (XDR-A. baumannii). 24 XDR-A. baumannii strains were isolated from patients' specimens. Broth microdilution assay was used to
Y Onodera et al.
The Journal of antimicrobial chemotherapy, 44(4), 533-536 (1999-12-10)
The in-vitro inhibitory activities of sitafloxacin (DU-6859a) and other quinolones against Streptococcus pneumoniae DNA gyrase and topoisomerase IV were measured. IC50s of levofloxacin, ciprofloxacin, sparfloxacin and tosufloxacin against DNA gyrase were almost three to 12 times higher than those against
David Leif Anderson
Drugs of today (Barcelona, Spain : 1998), 44(7), 489-501 (2008-09-23)
Sitafloxacin hydrate (DU-6859a, Gracevit), a new-generation, broad-spectrum oral fluoroquinolone that is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract

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