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Merck
모든 사진(1)

주요 문서

SML2744

Sigma-Aldrich

Sitafloxacin sesquihydrate

≥98% (HPLC)

동의어(들):

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

실험식(Hill 표기법):
C19H18ClF2N3O3·1.5H2O
CAS Number:
Molecular Weight:
436.84
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

양식

powder

저장 조건

desiccated

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

−20°C

SMILES string

F[C@@H]1[C@@H](C1)N2c3c(cc(c(c3Cl)N4C[C@H](C5(C4)CC5)N)F)C(=O)C(=C2)C(=O)O.O

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

InChI key

ANCJYRJLOUSQBW-JJZGMWGRSA-N

생화학적/생리학적 작용

Orally active, 4th generation fluoroquinolone broad-spectrum antibiotic with dual DNA gyrase and topoisomerase IV inhibitory activity.
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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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시험 성적서(COA)

Lot/Batch Number

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문서 라이브러리 방문

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
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
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
K Sato et al.
Antimicrobial agents and chemotherapy, 36(7), 1491-1498 (1992-07-01)
DU-6859, (-)-7-[(7S)-amino-5-azaspiro(2,4)heptan-5-yl]-8-chloro-6- fluoro-1-[(1R,2R)-cis-2-fluoro-1-cyclopropyl]-1,4-dihydro-4-oxoquinol one-3- carboxylic acid, is a new fluoroquinolone with antibacterial activity which is significantly better than those of currently available quinolones. The MICs for 90% of methicillin-susceptible and -resistant Staphylococcus aureus and Staphylococcus epidermidis clinical isolates (MIC90s) were

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