1. Anti-infection
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    Topoisomerase
    Antibiotic
  3. Gatifloxacin sesquihydrate

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

Cat. No.: HY-10581C
Handling Instructions

Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate 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 sesquihydrate can be used to treat bacterial conjunctivitis in vivo.

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

Gatifloxacin sesquihydrate Chemical Structure

Gatifloxacin sesquihydrate Chemical Structure

CAS No. : 180200-66-2

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Description

Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate 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 sesquihydrate can be used to treat bacterial conjunctivitis in vivo.

IC50 & Target

Topoisomerase II

36.7 μM (IC50)

In Vitro

Gatifloxacin sesquihydrate 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 sesquihydrate 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 sesquihydrate 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 sesquihydrate 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 sesquihydrate has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml)[2].
Gatifloxacin sesquihydrate (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 sesquihydrate, respectively[3].

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

In Vivo

Gatifloxacin sesquihydrate (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[4]
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

402.43

Formula

C₁₉H₂₂FN₃O₄.₃/₂H₂O

CAS No.

180200-66-2

SMILES

[H]O[H].O=C(C1=CN(C2CC2)C3=C(C=C(F)C(N4CC(C)NCC4)=C3OC)C1=O)O.[3/2]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

Gatifloxacin sesquihydrateAM-1155 sesquihydrateBMS-206584 sesquihydratePD135432 sesquihydrateBacterialTopoisomeraseAntibioticE. coli,?Pseudomonas aeruginosa,?Micrococcus luteusS. aureushypoglycemiahyperglycemiadiabeticactinomycetomaN. brasiliensisbacterialconjunctivitisInhibitorinhibitorinhibit

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