An ophthalmologic fluoroquinolone antibiotic
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Besifloxacin (hydrochloride)

Item No. 23692

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-[(3R)-3-aminohexahydro-1H-azepin-1-yl]-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid, monohydrochloride
CAS Number
405165-61-9
Synonyms
  • BOL-303224-A
Molecular Formula
C19H21ClFN3O3 • HCl
Formula Weight
430.3
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Methanol: 1 mg/mL*
SMILES
FC1=CC2=C(C(Cl)=C1N3C[C@H](N)CCCC3)N(C4CC4)C=C(C(O)=O)C2=O.Cl
InChi Code
InChI=1S/C19H21ClFN3O3.ClH/c20-15-16-12(18(25)13(19(26)27)9-24(16)11-4-5-11)7-14(21)17(15)23-6-2-1-3-10(22)8-23;/h7,9-11H,1-6,8,22H2,(H,26,27);1H/t10-;/m1./s1
InChi Key
PMQBICKXAAKXAY-HNCPQSOCSA-N
Shipping & Storage Information
Storage
4°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Besifloxacin is an ophthalmologic fluoroquinolone antibiotic that is active against Gram-negative and Gram-positive aerobic and anaerobic bacterial strains (MICs = 0.006-1.56 μg/ml).1 It inhibits LPS-stimulated production of the inflammatory cytokines IL-1β, IL-8, IL-6, and IL-1α in human THP-1 monocytes.2 Besifloxacin, when 2 drops of a 0.6% solution are applied per eye, yields a concentration of 2 μg/g which is greater than the MIC90s of ophthalmologic isolates of H. influenzae, S. pneumoniae, S. aureus, and Corynebacterium and reduces the number of bacteria found in the aqueous, but not vitreous, humor in a rabbit model of bacterial endophthalmitis.1,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ward, K.W., Lepage, J.F., and Driot, J.Y. Nonclinical pharmacodynamics, pharmacokinetics, and safety of BOL-303224-A, a novel fluoroquinolone antimicrobial agent for topical ophthalmic use. J. Ocul. Pharmacol. Ther. 23(3), 243-256 (2007).

    2. Zhang, J.-Z., and Ward, K.W. Besifloxacin, a novel fluoroquinolone antimicrobial agent, exhibits potent inhibition of pro-inflammatory cytokines in human THP-1 monocytes. J. Antimicrob. Chemother. 61(1), 111-116 (2008).

    3. Norcross, E.W., Sanders, M.E., Moore, Q., III, et al. Comparative efficacy of besifloxacin and other fluoroquinolones in a prophylaxis model of penicillin-resistant Streptococcus pneumoniae rabbit endophthalmitis. J. Ocul. Pharmacol. Ther. 26(3), 237-243 (2010).