Gatifloxacin
Based on 4 publication(s) in Google Scholar
Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic that can cross the blood-brain barrier, with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50=0.109 μg/ml). Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
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- Pureté : 99.69%
- CAS No.: 112811-59-3
- Formule: C19H22FN3O4
- Masse moléculaire:375.39
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Stockage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Quinolone |
Topoisomerase II 36.7 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
400 μM
Compound: Gatifloxacin
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Inhibition of human HeLa cell proliferation
Inhibition of human HeLa cell proliferation
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[PMID: 19595598] |
| HEp-2 | CC50 |
67 μM
Compound: gatifloxacin
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Cytotoxicity against human Hep2 laryngeal carcinoma cell line
Cytotoxicity against human Hep2 laryngeal carcinoma cell line
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[PMID: 16337791] |
| MDCK | CC50 |
396 μM
Compound: GTFX
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Cytotoxicity against MDCK cells after 48 hrs by CPE assay
Cytotoxicity against MDCK cells after 48 hrs by CPE assay
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[PMID: 21481984] |
| MRC5 | IC50 |
12.7 μM
Compound: GTFX (gatifloxacin)
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In vitro inhibitory activity on MRC5 fibroblast tissue cultures inoculated with virulent RH strain of Toxoplasma gondii
In vitro inhibitory activity on MRC5 fibroblast tissue cultures inoculated with virulent RH strain of Toxoplasma gondii
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[PMID: 15125930] |
| NIH3T3 | IC50 |
596 μM
Compound: 5
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Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by MTT assay
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[PMID: 18950903] |
| T-cell | IC50 |
>50 μg/mL
Compound: GTX
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Anti-inflammatory activity in Homo sapiens (human) T lymphocytes assessed as inhibition of PHA-induced [3H] thymidine uptake incubated for 72 hr prior to [3H]thymidine addition measured after 18 hr by liquid scintillation method
Anti-inflammatory activity in Homo sapiens (human) T lymphocytes assessed as inhibition of PHA-induced [3H] thymidine uptake incubated for 72 hr prior to [3H]thymidine addition measured after 18 hr by liquid scintillation method
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10.1007/s00044-009-9264-y |
| V79 | IC50 |
85 μg/mL
Compound: 10c
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Clonogenic cytotoxicity against Chinese hamster V-79 cells
Clonogenic cytotoxicity against Chinese hamster V-79 cells
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[PMID: 7473575] |
| Vero | CC50 |
>155.3 μM
Compound: Gati
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Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
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[PMID: 18502542] |
| Vero | CC50 |
125 μg/mL
Compound: GTFX
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 28646656] |
| Vero | CC50 |
125 μg/mL
Compound: GTFX
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 28720502] |
| Vero | CC50 |
64 μg/mL
Compound: Gatifloxacin
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Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay
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[PMID: 31352245] |
| Vero | IC50 |
>155.3 μM
Compound: Gati
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Cytotoxicity against Vero cells after 72 hrs by MTT assay
Cytotoxicity against Vero cells after 72 hrs by MTT assay
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[PMID: 17960928] |
| Vero | IC50 |
>155.3 μM
Compound: Gati
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Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
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[PMID: 18304818] |
| Vero | IC50 |
>155.3 μM
Compound: gatifloxacin
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Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
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[PMID: 18078756] |
| Vero | IC50 |
>159.5 μM
Compound: Gatifloxacin
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Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr
Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr
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10.1007/s00044-010-9322-5 |
| Vero | IC50 |
>550 μM
Compound: Gatifloxacin
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Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr by MTT assay
Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr by MTT assay
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10.1007/s00044-011-9646-9 |
| Vero | IC50 |
>62.5 μg/mL
Compound: Gati
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Cytotoxicity against Vero cell line
Cytotoxicity against Vero cell line
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[PMID: 16759086] |
In Vitro
Gatifloxacin is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with IC50 values of 13.8 μg/ml, 0.109 μg/ml, and 265 μg/ml, respectively[1].Gatifloxacin is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with MIC values of 0.05 μg/ml, 0.0063 μg/ml, and 122 μg/ml, respectively[1].Gatifloxacin exhibits antibacterial activities for wild-type strains (MS5935, MS5952, MR5867 and MR6009) the first-, second-, third-, and fourth-step mutants with MIC values of 0.05 to 0.10 μg/ml, 0.20 μg/ml, 1.56 to 3.13 μg/ml, 1.56 to 6.25 μg/ml, and 50 to 200 μg/ml, respectively. Gatifloxacin displays the most potent activity against the second- and third-step mutants (MS5952, MR5867 and MR6009) except for the second-step mutant of strain MS5935[2]. Gatifloxacin has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml)[2].Gatifloxacin (20-100 μM; 72 hours) significantly decreases insulin content to 60% at Day 1, and continues to be reduced to 50.1% and 44.7% at Day 3 by 20 μM and 100 μM gatifloxacin, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice with Nocardia brasiliensis in the right hind footpad.
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Dosage:100 mg/kg
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Administration:Subcutaneous injection; 3 times a day; 30 days
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Result:Reduced the production of lesions in mice.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 112811-59-3
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Appearance Solid
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Masse moléculaire 375.39
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Formule C19H22FN3O4
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Color White to off-white
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SMILES
CC1NCCN(C2=C(F)C=C3C(N(C4CC4)C=C(C(O)=O)C3=O)=C2OC)C1
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Synonyms
AM-1155; BMS-206584; PD135432
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (4)
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Journal Impact Factor
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Most Recent
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J Appl Toxicol
Reactive metabolite of trovafloxacin activates inflammasomes: Implications for trovafloxacin-induced liver injury. [Abstract]2024 Jun;44(6):846-852. PMID: 38291012 -
Ghent university
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Solvant et solubilité
In Vitro:
DMSO : 2 mg/mL (5.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (2.66 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Takei M, et al. Inhibitory activities of gatifloxacin (AM-1155), a newly developed fluoroquinolone, against bacterial and mammalian type II topoisomerases.Antimicrob Agents Chemother. 1998 Oct;42(10):2678-81. [Content Brief]
[2]. Fukuda H, et al. Antibacterial activity of gatifloxacin (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus. Antimicrob Agents Chemother. 1998 Aug;42(8):1917-22. [Content Brief]
[3]. Yamada C, et al. Gatifloxacin acutely stimulates insulin secretion and chronically suppresses insulin biosynthesis. Eur J Pharmacol. 2006 Dec 28;553(1-3):67-72. Epub 2006 Sep 28. [Content Brief]
[4]. Lutsar I, et al. Pharmacodynamics of gatifloxacin in cerebrospinal fluid in experimental cephalosporin-resistant pneumococcal meningitis. Antimicrob Agents Chemother. 1998 Oct;42(10):2650-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.6639 mL | 13.3195 mL | 26.6390 mL | 66.5974 mL |
| DMSO | 5 mM | 0.5328 mL | 2.6639 mL | 5.3278 mL | 13.3195 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Gatifloxacin Related Classifications
HY-10581 Related Classifications
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Keywords
- Gatifloxacin
- 112811-59-3
- AM-1155
- BMS-206584
- PD135432
- AM1155
- AM 1155
- BMS206584
- BMS 206584
- BMS-206584
- PD135432
- PD 135432
- PD-135432
- Bacterial
- Topoisomerase
- Antibiotic
- E. coli
- Pseudomonas aeruginosa
- Micrococcus luteus
- S. aureus
- hypoglycemia
- hyperglycemia
- diabetic
- actinomycetoma
- N. brasiliensis
- bacterial
- conjunctivitis
- Inhibitor
- inhibitor
- inhibit