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
- Molecular Weight:
- 409.81
- MDL Number:
- MFCD00903720
- MOL File:
- 127254-12-0.mol
- MSDS File:
- SDS
| 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) |
| FDA UNII | 3GJC60U4Q8 |
| ATC code | J01MA21 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
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|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501 | |||||||||
| NFPA 704 |
|
Sitafloxacin price More Price(7)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| American Custom Chemicals Corporation | API0006381 | SITAFLOXACIN 95.00% | 127254-12-0 | 1G | $3405.15 | 2021-12-16 | Buy |
| Matrix Scientific | 120731 | 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 97% | 127254-12-0 | 1g | $3960 | 2021-12-16 | Buy |
| Matrix Scientific | 120731 | 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 97% | 127254-12-0 | 5g | $11880 | 2021-12-16 | Buy |
| Crysdot | CD31004021 | Sitafloxacin 98+% | 127254-12-0 | 5mg | $88 | 2021-12-16 | Buy |
| Crysdot | CD31004021 | Sitafloxacin 98+% | 127254-12-0 | 10mg | $166 | 2021-12-16 | Buy |
Sitafloxacin Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Yingrui Biopharma Co., Ltd. | +86-21-33585366 - 03@ | sales03@shyrchem.com | CHINA | 738 | 60 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Shanghai Yingrui Biopharma Co.,Ltd | 21-33585366 | export01@shyrchem.com | CHINA | 1320 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 47465 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| Shaanxi Dideu Medichem Co. Ltd | 18192627656 | 1012@dideu.com | China | 3657 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29474 | 58 |
| AFINE CHEMICALS LIMITED | 0571-85134551 | info@afinechem.com | CHINA | 15377 | 58 |
| Baoji Guokang Bio-Technology Co., Ltd. | 0917-3909592 13892490616 | gksales1@gk-bio.com | China | 9339 | 58 |
| Baoji Guokang Healthchem co.,ltd | +8615604608665 15604608665 | dominicguo@gk-bio.com | CHINA | 9427 | 58 |
Related articles
- Side-effects of Sitafloxacin
- Sitafloxacin (as sitafloxacin hydrate) is available as 50-mg tablets, under the name Gracevit, and as a 10% fine granular prep....
- Mar 23，2022
View Lastest Price from Sitafloxacin manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2023-06-26 | Sitafloxacin
127254-12-0
|
US $200.00 / kg | 1kg | 99% | 1000kg/Months | Hebei Mingeng Biotechnology Co., Ltd | |
 |
2023-03-29 | Sitafloxacin
127254-12-0
|
US $50.00 / kg | 1kg | 99% | 20 tons | Hebei Duling International Trade Co. LTD | |
 |
2021-07-20 | Sitafloxacin USP/EP/BP
127254-12-0
|
US $1.10 / g | 1g | 99.9% | 100 Tons Min | Dideu Industries Group Limited |
-
- Sitafloxacin
127254-12-0
- US $200.00 / kg
- 99%
- Hebei Mingeng Biotechnology Co., Ltd
-
- Sitafloxacin
127254-12-0
- US $50.00 / kg
- 99%
- Hebei Duling International Trade Co. LTD
-
- Sitafloxacin USP/EP/BP
127254-12-0
- US $1.10 / g
- 99.9%
- Dideu Industries Group Limited
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