Balofloxacin

• CAT Number: A000522
• CAS Number: 127294-70-6
• Molecular Formula: C20H24FN3O4
• Molecular Weight: 389.42
• Purity: ≥95%
• Synonyms: 127294-70-6; 1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-(methylamino)piperidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid; Balofloxacin [INN]; Baloxin; Q 35
• Target: Bacterial
• Solubility: Soluble in DMSO > 10 mM
• Storage: -20°C
• IUPAC Name: 1-cyclopropyl-6-fluoro-8-methoxy-7-[3-(methylamino)piperidin-1-yl]-4-oxoquinoline-3-carboxylic acid
• InChI: InChI=1S/C20H24FN3O4/c1-22-11-4-3-7-23(9-11)17-15(21)8-13-16(19(17)28-2)24(12-5-6-12)10-14(18(13)25)20(26)27/h8,10-12,22H,3-7,9H2,1-2H3,(H,26,27)
• InChIKey: MGQLHRYJBWGORO-UHFFFAOYSA-N
• SMILES: CNC1CCCN(C1)C2=C(C=C3C(=C2OC)N(C=C(C3=O)C(=O)O)C4CC4)F

Balofloxacin（Cat No.:A000522）is a fluoroquinolone antibiotic primarily used to treat bacterial infections, particularly those affecting the urinary tract. It works by inhibiting bacterial DNA gyrase and topoisomerase IV, essential enzymes for DNA replication and transcription, leading to bacterial cell death. Known for its efficacy against Gram-negative bacteria like Escherichia coli and Klebsiella pneumoniae, Balofloxacin is also effective against certain Gram-positive strains. Its favorable pharmacokinetics and antibacterial spectrum make it a valuable option in managing persistent or resistant infections, especially in urinary and respiratory tract infections.

Reference

1: Chen XH, Zhang BW, Li H, Peng XX. Myo-inositol improves the host/’s ability to
eliminate balofloxacin-resistant Escherichia coli. Sci Rep. 2015 Jun 1;5:10720.
doi: 10.1038/srep10720. PubMed PMID: 26030712; PubMed Central PMCID: PMC5377236.

2: Jiang H, Han S, Guo C, Liu T, Wu X. In vitro and in vivo effectiveness
evaluation of balofloxacin in experimental Staphylococcus aureus keratitis. J
Ocul Pharmacol Ther. 2014 Aug;30(6):482-8. doi: 10.1089/jop.2013.0178. Epub 2014
May 14. PubMed PMID: 24828089.

3: Li H, Pan JY, Liu XJ, Gao JX, Wu HK, Wang C, Peng XX. Alterations of protein
complexes and pathways in genetic information flow and response to stimulus
contribute to Escherichia coli resistance to balofloxacin. Mol Biosyst. 2012
Sep;8(9):2303-11. Epub 2012 Jun 22. PubMed PMID: 22729160.

4: Li P, Liu X, Li H, Peng XX. Downregulation of Na(+)-NQR complex is essential
for Vibrio alginolyticus in resistance to balofloxacin. J Proteomics. 2012 May
17;75(9):2638-48. doi: 10.1016/j.jprot.2012.03.006. Epub 2012 Mar 17. PubMed
PMID: 22465713.

5: Feng LS, Liu ML, Wang B, Chai Y, Hao XQ, Meng S, Guo HY. Synthesis and in
vitro antimycobacterial activity of balofloxacin ethylene isatin derivatives. Eur
J Med Chem. 2010 Aug;45(8):3407-12. doi: 10.1016/j.ejmech.2010.04.027. Epub 2010
May 20. PubMed PMID: 20493593.

6: Betanzos-Cabrera G, Juárez-Verdayes MA, González-González G, Cancino-Díaz ME,
Cancino-Díaz JC. Gatifloxacin, moxifloxacin, and balofloxacin resistance due to
mutations in the gyrA and parC genes of Staphylococcus epidermidis strains
isolated from patients with endophthalmitis, corneal ulcers and conjunctivitis.
Ophthalmic Res. 2009;42(1):43-8. doi: 10.1159/000219684. Epub 2009 May 28. PubMed
PMID: 19478540.

7: Deng J, Xiao Z, Zhang H, Zhang M, Tang J. [Determination of balofloxacin in
human plasma by HPLC with solid-phase extraction]. Se Pu. 2007 Nov;25(6):942-3.
Chinese. PubMed PMID: 18257322.

8: Bian Z, Tian Y, Zhang Z, Xu F, Li J, Cao X. High performance liquid
chromatography-electrospray ionization mass spectrometric determination of
balofloxacin in human plasma and its pharmacokinetics. J Chromatogr B Analyt
Technol Biomed Life Sci. 2007 May 1;850(1-2):68-73. Epub 2006 Dec 11. PubMed
PMID: 17161665.

9: Yan ZY, Shao XF, Jiang XM, Hu YZ. [Studies on the reaction of balofloxacin
with bovine serum albumin]. Guang Pu Xue Yu Guang Pu Fen Xi. 2006
Aug;26(8):1494-8. Chinese. PubMed PMID: 17058955.

10: Seop Kim D, Kim KS, Hwan Choi K, Na H, Kim JI, Shin WH, Kim EJ.
Electrophysiological safety of novel fluoroquinolone antibiotic agents
gemifloxacin and balofloxacin. Drug Chem Toxicol. 2006;29(3):303-12. PubMed PMID:
16777708.