Synonym
Balofloxacin; Balofloxacin [INN]; Q 35; UNII-Q022B63JPM; Q-35; Q35;
IUPAC/Chemical Name
(+-)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-(methylamino)piperidino)-4-oxo-3-quinolinecarboxylic acid
InChi Key
MGQLHRYJBWGORO-UHFFFAOYSA-N
InChi Code
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)
SMILES Code
CNC1CCCN(C1)c2c(cc3c(c2OC)n(cc(c3=O)C(=O)O)C4CC4)F
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Balofloxacin (Q-35) is a fluoroquinolone antibiotic with broad-spectrum antibacterial activity against gram-negative, gram-positive, and anaerobic bacteria.
In vitro activity:
In vitro testing compared the cellular toxicity of and bacterial susceptibility to balofloxacin and levofloxacin in human corneal epithelial cells (HCECs). In vitro toxicity examinations showed that balofloxacin, as well as levofloxacin, had low cytotoxicity in HCECs. Balofloxacin eye drops (0.5%) also showed a similar relative cytotoxicity to levofloxacin eye drops (0.5%). In bacterial susceptibility examinations, both balofloxacin and levofloxacin significantly reduced S. aureus compared with the untreated control (P<0.001 for both balofloxacin and levofloxacin).
Reference: J Ocul Pharmacol Ther. 2014 Aug;30(6):482-8. https://www.liebertpub.com/doi/10.1089/jop.2013.0178?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub%20%200pubmed
In vivo activity:
For in vivo testing, experimental bacterial keratitis was induced and treated with balofloxacin eye drops (0.5%) and levofloxacin eye drops (0.5%). Balofloxacin was more effective than levofloxacin in the treatment of S. aureus bacterial keratitis (P<0.05). In experimental bacterial keratitis treatment testing, balofloxacin was also more effective than levofloxacin with respect to the parameters of physiological score, histological observation, and bacterial quantitation (P<0.05).
Reference: J Ocul Pharmacol Ther. 2014 Aug;30(6):482-8. https://www.liebertpub.com/doi/10.1089/jop.2013.0178?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub%20%200pubmed
|
Solvent |
mg/mL |
mM |
| Solubility |
| Water |
2.8 |
7.29 |
| DMSO |
0.8 |
2.16 |
| DMF |
10.0 |
25.68 |
| DMF:PBS (pH 7.2) (1:1) |
0.5 |
1.28 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
389.42
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. 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. PMID: 24828089.
In vitro protocol:
1. 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. PMID: 24828089.
In vivo protocol:
1. 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. PMID: 24828089.
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.
2: Ma X, Yan J, Wang Q, Wu D, Li H. Spectroscopy study and co-administration effect on the interaction of mycophenolic acid and human serum albumin. Int J Biol Macromol. 2015;77:280-6. doi: 10.1016/j.ijbiomac.2015.03.052. Epub 2015 Apr 1. PubMed PMID: 25841376.
3: 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.
4: 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.
5: 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.
6: 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.
