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

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.

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].

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

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].

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

402.43

C₁₉H₂₂FN₃O₄.3/2H₂O

180200-66-2

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

Room temperature in continental US; may vary elsewhere.

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

• [1]. Takei M, et al. Inhibitory activities of Gatifloxacin mesylate (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 mesylate (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 mesylate 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]. Daw-Garza A, et al. In vivo therapeutic effect of Gatifloxacin mesylate on BALB/c mice infected with Nocardia brasiliensis.Antimicrob Agents Chemother. 2008 Apr;52(4):1549-50.  [Content Brief]