Description References
ChemicalBook > CAS DataBase List > Sitafloxacin

Sitafloxacin

Description References
Product Name
Sitafloxacin
CAS No.
127254-12-0
Chemical Name
Sitafloxacin
Synonyms
spifloxacin;Sitfloxacfn;Sitafloxacfn;The west was;Sitafloxacin-d4;Sitafloxacin anhydrous;Sitafloxacin (DU-6859a);Sitafloxacin ABCDEFGHJKL;7-((S)-7-Amino-5-azaspiro[2.4]heptan-5-yl)-8-chloro-6-fluoro-1-((1R,2S)-2-fluorocyclopropyl)-4;7-[(7S)-7-amino-5-azaspiro[2.4]heptan-5-yl]-8-chloro-6-fluoro-1-[(2S)-2-fluorocyclopropyl]-4-oxoquinoline-3-carboxylicaci
CBNumber
CB8222468
Molecular Formula
C19H18ClF2N3O3
Formula Weight
409.81
MOL File
127254-12-0.mol
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Sitafloxacin Property

Boiling point:
629.2±55.0 °C(Predicted)
Density 
1.63±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: slightly soluble; DMSO: slightly soluble; Methanol: slightly soluble
form 
A crystalline solid
pka
6.39±0.50(Predicted)
CAS DataBase Reference
127254-12-0(CAS DataBase Reference)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

American Custom Chemicals Corporation
Product number
API0006381
Product name
SITAFLOXACIN
Purity
95.00%
Packaging
1G
Price
$3405.15
Updated
2021/12/16
Matrix Scientific
Product number
120731
Product name
7-((S)-7-Amino-5-azaspiro[2.4]heptan-5-yl)-8-chloro-6-fluoro-1-((1R,2S)-2-fluorocyclopropyl)-4-oxo-1,4-dihydroquinoline-3-carboxylicacid
Purity
97%
Packaging
1g
Price
$3960
Updated
2021/12/16
Matrix Scientific
Product number
120731
Product name
7-((S)-7-Amino-5-azaspiro[2.4]heptan-5-yl)-8-chloro-6-fluoro-1-((1R,2S)-2-fluorocyclopropyl)-4-oxo-1,4-dihydroquinoline-3-carboxylicacid
Purity
97%
Packaging
5g
Price
$11880
Updated
2021/12/16
Crysdot
Product number
CD31004021
Product name
Sitafloxacin
Purity
98+%
Packaging
5mg
Price
$88
Updated
2021/12/16
Crysdot
Product number
CD31004021
Product name
Sitafloxacin
Purity
98+%
Packaging
10mg
Price
$166
Updated
2021/12/16
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Sitafloxacin Chemical Properties,Usage,Production

Description

Sitafloxacin (Trade name: Gracevit in Japan) belongs to a new generation, broad-spectrum oral fluoroquinolone antibiotics. It is highly active against various kinds of gram-negative, gram-positive and anaerobic clinical isolates, even including strains that are resistant to other kinds of fluoroquinolone antibiotics. It has been listed in Japan for the treatment of respiratory and urinary tract infections. It also shows potential for the treatment of Buruli ulcer. Its mechanism of action is through inhibiting the Topoisomerase II ligase domain of bacteria, causing DNA fragmentation to inhibit the DNA synthesis of bacteria.

References

http://www.biochempartner.com/product_details.aspx?item_id=6084
https://en.wikipedia.org/wiki/Sitafloxacin

Description

Sitafloxacin hydrate is the newest member (fourth generation) of the fluoroquinolone family of antibiotics that exhibits broad spectrum activity against many Gram-positive, Gramnegative, and anaerobic clinical isolates, including strains resistant to other fluoroquinolones. Since the launch of the first fluoroquinolone norfloxacin (patented in 1978), 20 other versions have made it to market with ciprofloxacin and levofloxacin experiencing the most prevalent usage. The mechanism of action involves inhibition of bacterial type II topoisomerases, both DNA gyrase and topoisomerase IV. By inhibiting these enzymes and preventing DNA supercoiling, cell division is disrupted leading to cell death. In Gram-negative bacteria, the primary target appears to be gyrase, whereas topoisomerase IV is involved in Gram-positive bacteria. Dual inhibition is attractive for widespread activity and avoidance of resistance as both encoding genes would have to acquire mutations.

Originator

Daiichi Sankyo (Japan)

Uses

Antibacterial (DNA-gyrase inhibitor).

Definition

ChEBI: Sitafloxacin is a member of quinolines, a quinolone antibiotic and a fluoroquinolone antibiotic.

brand name

Gracevit

Pharmaceutical Applications

A group 4 quinolone formulated for oral or intravenous use. In-vitro activity is similar to or better than that of moxifloxacin. The antibacterial spectrum covers Gram-positive and Gram-negative bacteria including anaerobes. It has a chlorine atom at the C-8 position, and therefore has potential for phototoxicity. Early interest in this compound has not been maintained, but it is available in Japan.

Side effects

As a class, the major adverse events for fluoroquinolones are cardiac arrhythmia (due to QT interval 622 Shridhar Hegde and Michelle Schmidt prolongation), major phototoxicity, CNS disturbances (seizures, dizziness, and headaches), and tendonitis. The GI side effects, common to most antimicrobials, include Clostridium difficile-associated diarrhea (CDAD) and alterations in glucose homeostasis. From the clinical safety profile of sitafloxacin (1,059 patients receiving either 50 mg b.i.d. or 100 mg b.i.d.), about a third of patients experienced an adverse event with the most common being diarrhea, liver enzyme elevations, and headaches; however, the risk of QT prolongation, hypoglycemia, and hepatotoxicity were all considered to be low. Phototoxicity appears to be the limiting toxicity, particularly in non-Asian patients.

Sitafloxacin Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Sitafloxacin manufacturers

Hebei Duling International Trade Co. LTD
Product
Sitafloxacin 127254-12-0
Price
US $50.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
20 tons
Release date
2023-03-29
Hebei Mingeng Biotechnology Co., Ltd
Product
Sitafloxacin 127254-12-0
Price
US $200.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
1000kg/Months
Release date
2022-11-20
Dideu Industries Group Limited
Product
Sitafloxacin 127254-12-0
Price
US $1.10/g
Min. Order
1g
Purity
99.9%
Supply Ability
100 Tons Min
Release date
2021-07-19

127254-12-0, SitafloxacinRelated Search:


  • spifloxacin
  • 7-[(4S)-4-Amino-6-azaspiro[2.4]heptan-6-yl]-8-chloro-6-fluoro-1-[(2S)-2-fluorocyclopropyl]-4-oxoquinoline-3-carboxylic acid
  • 3-Quinolinecarboxylic acid, 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-
  • Sitafloxacin anhydrous
  • 7-((S)-7-Amino-5-azaspiro[2.4]heptan-5-yl)-8-chloro-6-fluoro-1-((1R,2S)-2-fluorocyclopropyl)-4
  • Sitafloxacfn
  • Sitfloxacfn
  • Sitafloxacin-d4
  • Sitafloxacin ABCDEFGHJKL
  • 7-[(7S)-7-amino-5-azaspiro[2.4]heptan-5-yl]-8-chloro-6-fluoro-1-[(2S)-2-fluorocyclopropyl]-4-oxoquinoline-3-carboxylic acid
  • Sitafloxacin (DU-6859a)
  • 7-((S)-7-Amino-5-azaspiro[2.4]heptan-5-yl)-8-chloro-6-fluoro-1-((1R,2S)-2-fluorocyclopropyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
  • The west was
  • 7-[(7S)-7-amino-5-azaspiro[2.4]heptan-5-yl]-8-chloro-6-fluoro-1-[(2S)-2-fluorocyclopropyl]-4-oxoquinoline-3-carboxylicaci
  • 127254-12-0
  • C19H18ClF2N3O3
  • intermediates