Gemifloxacin
Gemifloxacin, a fluoroquinolone, is a potent and orally active antipneumococcal agent. Gemifloxacin shows bactericidal activity against highly quinolone-resistant pneumococci.Gemifloxacin can be used for the research of respiratory infections, such as community-acquired pneumonia (CAP) and acute exacerbation of chronic bronchitis (AECB).
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- CAS No.: 175463-14-6
- Formule: C18H20FN5O4
- Masse moléculaire:389.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
|
Quinolone |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEp-2 | CC50 |
46 μM
Compound: GEM
|
Cytotoxicity against human Hep2 cell line after 72 hrs
Cytotoxicity against human Hep2 cell line after 72 hrs
|
[PMID: 17228862] |
| HEp-2 | CC50 |
46 μM
Compound: GEM
|
Cytotoxicity against human Hep2 cell line after 72 hrs
Cytotoxicity against human Hep2 cell line after 72 hrs
|
[PMID: 21443219] |
| HEp-2 | CC50 |
46 μM
Compound: gemifloxacin
|
Cytotoxicity against human Hep2 laryngeal carcinoma cell line
Cytotoxicity against human Hep2 laryngeal carcinoma cell line
|
[PMID: 16337791] |
| Hepatocyte | CC50 |
>100 μM
Compound: GEM
|
Cytotoxicity against rat hepatocytes after 48 hrs
Cytotoxicity against rat hepatocytes after 48 hrs
|
[PMID: 17228862] |
| HepG2 | CC50 |
35 μM
Compound: GEM
|
Cytotoxicity against human HepG2 cells after 72 hrs
Cytotoxicity against human HepG2 cells after 72 hrs
|
[PMID: 17228862] |
| HepG2 | IC50 |
13.49 μg/mL
Compound: Gemifloxacin (GMFX)
|
Cytotoxicity was determined for the compound in HepG2 cell line
Cytotoxicity was determined for the compound in HepG2 cell line
|
[PMID: 14980680] |
| MDCK | CC50 |
321 μM
Compound: GMFX
|
Cytotoxicity against MDCK cells after 48 hrs by CPE assay
Cytotoxicity against MDCK cells after 48 hrs by CPE assay
|
[PMID: 21481984] |
| V79-4 | IC50 |
10.08 μg/mL
Compound: Gemifloxacin (GMFX)
|
Cytotoxicity was determined for the compound in V79-4 cell line
Cytotoxicity was determined for the compound in V79-4 cell line
|
[PMID: 14980680] |
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 175463-14-6
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Masse moléculaire 389.38
-
Formule C18H20FN5O4
-
SMILES
NCC(C1)/C(CN1C(N=C2C(C(C(C(O)=O)=CN2C3CC3)=O)=C4)=C4F)=N/OC
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Synonyms
SB-265805; LB20304
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Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Bacterial live/dead nucleic-acid viability staining
The LIVE/DEAD bacterial viability staining method is based on differential permeability of nucleic-acid-binding fluorescent dyes, most commonly SYTO 9 and propidium iodide (PI), which enables discrimination of bacterial populations with intact versus compromised cytoplasmic membranes. SYTO 9 penetrates both intact and damaged bacterial membranes and binds nucleic acids to produce green fluorescence, whereas propidium iodide penetrates only cells with compromised membranes and fluoresces red while also reducing SYTO 9 signal through competitive binding and fluorescence interactions. The resulting fluorescence pattern is interpreted as a proxy for membrane integrity, which is widely used as an indicator of bacterial viability in microscopy, flow cytometry, and spectroscopic platforms. However, mechanistic studies show that SYTO 9 and PI interactions involve displacement and fluorescence resonance energy transfer effects, which can influence signal interpretation depending on dye ratios a
Pureté et documentation
Références
[1]. Yoo BK, et al. Gemifloxacin: a new fluoroquinolone approved for treatment of respiratory infections. Ann Pharmacother. 2004 Jul-Aug;38(7-8):1226-35. [Content Brief]
[2]. Davies TA, et al. Antipneumococcal activities of gemifloxacin compared to those of nine other agents. Antimicrob Agents Chemother. 2000 Feb;44(2):304-10. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)