1. Anti-infection
    Cell Cycle/DNA Damage
  2. Bacterial
    Topoisomerase
    Antibiotic
  3. Gatifloxacin

Gatifloxacin (Synonyms: AM-1155; BMS-206584; PD135432)

Cat. No.: HY-10581 Purity: 99.37%
Handling Instructions

Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic 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.

For research use only. We do not sell to patients.

Gatifloxacin Chemical Structure

Gatifloxacin Chemical Structure

CAS No. : 112811-59-3

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Based on 2 publication(s) in Google Scholar

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Description

Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic 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)[1]. Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.

IC50 & Target

Topoisomerase II

36.7 μM (IC50)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Gatifloxacin (subcutaneous injection; 100 mg/kg; 3 times a day; 30 days) significantly decreases the number of lesions in mouse footpad with Nocardia brasiliensis[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c mice with Nocardia brasiliensis in the right hind footpad.
Dosage: 100 mg/kg
Administration: Subcutaneous injection; 3 times a day; 30 days
Result: Reduced the production of lesions in mice.
Clinical Trial
Molecular Weight

375.39

Formula

C₁₉H₂₂FN₃O₄

CAS No.

112811-59-3

SMILES

CC1NCCN(C2=C(F)C=C3C(N(C4CC4)C=C(C(O)=O)C3=O)=C2OC)C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (5.33 mM; Need ultrasonic)

H2O : 1 mg/mL (2.66 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6639 mL 13.3195 mL 26.6390 mL
5 mM 0.5328 mL 2.6639 mL 5.3278 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

GatifloxacinAM-1155 BMS-206584 PD135432AM1155AM 1155BMS206584BMS 206584BMS-206584PD135432PD 135432PD-135432BacterialTopoisomeraseAntibioticE. coli,?Pseudomonas aeruginosa,?Micrococcus luteusS. aureushypoglycemiahyperglycemiadiabeticactinomycetomaN. brasiliensisbacterialconjunctivitisInhibitorinhibitorinhibit

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