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Chemical Structure| 163253-35-8 Chemical Structure| 163253-35-8

Structure of Sitafloxacin hydrate
CAS No.: 163253-35-8

Chemical Structure| 163253-35-8

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Sitafloxacin Hydrate is a fluoroquinolone antibiotic with promising effect on the treatment of Buruli ulcer.

Synonyms: DU-6859a; DU6859a hydrate; Sitafloxacin(hydrate)

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Product Details of Sitafloxacin hydrate

CAS No. :163253-35-8
Formula : C38H42Cl2F4N6O9
M.W : 873.67
SMILES Code : O=C(O)C1=CN(C2=C(C1=O)C=C(C(N(CC34CC4)C[C@H]3N)=C2Cl)F)[C@H]5[C@H](C5)F.[H]O[H].O=C(O)C6=CN(C7=C(C6=O)C=C(C(N(CC89CC9)C[C@H]8N)=C7Cl)F)[C@H]%10[C@H](C%10)F.[H]O[H].[H]O[H]
Synonyms :
DU-6859a; DU6859a hydrate; Sitafloxacin(hydrate)
MDL No. :MFCD11046360

Safety of Sitafloxacin hydrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Mycobacterium avium complex (MAC) 0.0625–64 μg/mL Evaluate the in vitro activity of STFX against MAC PMC6519390
Colistin-resistant Acinetobacter baumannii (CoR-AB) 0.02–8 mg/L 18 hours Evaluate the antibacterial activity of Sitafloxacin against CoR-AB, results showed 95.4% of CoR-AB were susceptible to Sitafloxacin. PMC7459680
Carbapenem-resistant Acinetobacter baumannii (CRAB) 0.02–8 mg/L 18 hours Evaluate the antibacterial activity of Sitafloxacin against CRAB, results showed 96.5% of CRAB were susceptible to Sitafloxacin. PMC7459680
Multidrug-resistant Acinetobacter baumannii (MDR-AB) 0.02–8 mg/L 18 hours Evaluate the antibacterial activity of Sitafloxacin against MDR-AB, results showed 96.6% of MDR-AB were susceptible to Sitafloxacin. PMC7459680
Gram-positive cocci 0.008-8 μg/ml (MIC) 20-24 hours Sitafloxacin exhibited good activity against staphylococci and streptococci, with an MIC90 of 0.5 μg/ml for methicillin-resistant Staphylococcus aureus. PMC89825
Gram-negative bacteria 0.008-4 μg/ml (MIC) 20-24 hours Sitafloxacin's activity against Enterobacteriaceae and nonfermenters was either equivalent to or better than that of clinafloxacin, inhibiting 96.9% of the strains at 1 μg/ml. PMC89825
THP-1 cells 50 µg/mL 4 hours To evaluate the inhibitory effect of Sitafloxacin on TNFα release in LPS-stimulated THP-1 cells. Results showed that Sitafloxacin reduced TNFα release by suppressing TACE phosphorylation and activity. PMC8683466
Macrophages 0.2, 1, 5, 10 mg/L 4, 24, 48 hours To evaluate the inhibitory effect of Sitafloxacin on intracellular M. abscessus growth, results showed comparable efficacy to clarithromycin and superior to moxifloxacin at certain concentrations. PMC8770805
Anaerobes 0.008-16 μg/ml (MIC) 48 hours Sitafloxacin demonstrated good activity against anaerobic bacteria, inhibiting 96.3% of the strains at 1 μg/ml. PMC89825
Helicobacter pylori 0.002–0.5 μg/mL 72 hours Evaluate the in vitro activity of sitafloxacin against H. pylori, showing the highest antibacterial activity (MIC90, 0.06 μg/ml) PMC3165289
Helicobacter pylori ≤0.5 μg/mL 72 hours To evaluate the antibacterial activity of Sitafloxacin against Helicobacter pylori, including strains with gyrA gene mutations. Results showed MICs of ≤0.5 μg/ml for all isolates. PMC2704646
Neisseria gonorrhoeae 0.004 to 2 mg/L (MIC) Evaluate the in vitro activity of Sitafloxacin against drug-resistant N. gonorrhoeae, with MIC50 and MIC90 of 0.125 mg/L and 0.5 mg/L, respectively PMC11118021
Helicobacter pylori 0.008 mg/L (MIC90) Compared the in vitro activities of Sitafloxacin with other quinolones against H. pylori strains with gyrA mutations, showing that Sitafloxacin had the most potent activity. PMC2663081

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mongolian gerbils H. pylori ATCC 43504 infection model Oral 0.3, 1, 3 mg/kg Twice daily for one week Evaluate the eradication effect of sitafloxacin alone or in combination with lansoprazole on H. pylori, showing a therapeutic rate of 83.3% for the combination PMC3165289

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.14mL

0.23mL

0.11mL

5.72mL

1.14mL

0.57mL

11.45mL

2.29mL

1.14mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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