Gatifloxacin sesquihydrate
Based on 4 publication(s) in Google Scholar
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.
- CAS No.: 180200-66-2
- Formula: C19H22FN3O4.3/2H2O
- Molecular Weight:402.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Gatifloxacin sesquihydrate
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Biological Activity
Description
IC50 & Target
[1]|
Quinolone |
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].
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[4]
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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.
Chemical Information
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CAS No. 180200-66-2
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Molecular Weight 402.43
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Formula C19H22FN3O4.3/2H2O
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SMILES
[H]O[H].O=C(C1=CN(C2CC2)C3=C(C=C(F)C(N4CC(C)NCC4)=C3OC)C1=O)O.[3/2]
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Synonyms
AM-1155 sesquihydrate; BMS-206584 sesquihydrate; PD135432 sesquihydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Gatifloxacin sesquihydrate
- 180200-66-2
- AM-1155 sesquihydrate
- BMS-206584 sesquihydrate
- PD135432 sesquihydrate
- Bacterial
- Topoisomerase
- Antibiotic
- E. coli
- Pseudomonas aeruginosa
- Micrococcus luteus
- S. aureus
- hypoglycemia
- hyperglycemia
- diabetic
- actinomycetoma
- N. brasiliensis
- bacterial
- conjunctivitis
- Inhibitor
- inhibitor
- inhibit