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KB-5246

Catalog No.GC32334 Copy One-Click Copy Product Info

KB-5246 is a tetracyclic quinolone and displays antibacterial activities.

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KB-5246 Chemical Structure

Cas No.: 119474-55-4

Size Price Stock Qty
1mg
$1,381.00
In stock
5mg
$2,210.00
In stock
10mg
$3,537.00
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Sample solution is provided at 25 µL, 10mM.



Description of KB-5246

KB-5246 is a tetracyclic quinolone and displays antibacterial activities.

KB-5246 is a tetracyclic quinolone and displays antibacterial activities. The MICs for 90% of isolates tested (MIC90s) of KB-5246 against gram-positive microorganisms such as Staphylococcus aureus, including methicillin-resistant S. aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, and Streptococcus pyogenes, are 0.39 μg/mL. KB5246 inhibits 90% of isolates of Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca at a concentration of 0.10 μg/mL or less. When a concentration of KB-5246 at the MIC or higher is added, no regrowth after 24 h of incubation is observed[1].

The 50% effective dose values of KB-5246 against S. pneumoniae 2132 infections are 50.5 mg/kg of body weight. The activities of KB-5246 against S. aureus Smith, P. aeruginosa GN11189, and Serratia marcescens GN7577 infections are comparable to those of ofloxacin and greater than those of norfloxacin[1].

[1]. Kotera Y, et al. In vitro and in vivo antibacterial activities of KB-5246, a new tetracyclic quinolone. Antimicrob Agents Chemother. 1989 Nov;33(11):1896-900.

Protocol of KB-5246

Cell experiment:

Bactericidal activity is tested by evaluating the reduction of viable cells during exposure to KB-5246 for 24 h. An overnight culture of microorganisms in sensitivity test broth is diluted to about 104 CFU/mL in the same medium and incubated at 37°C on a shaker. After 2 h of incubation, KB-5246 is added to the cultures at final concentrations of one half, one, two, or four times the MIC[1].

Animal experiment:

In vivo antibacterial activity against systemic infections in mice is determined. Ten male ddY mice weighing 19 to 23 g each are used for each dose level. An overnight culture in brain heart infusion broth at 37°C is diluted appropriately in the same medium with 4% gastrin mucin. A 0.2 mL sample of a bacterial suspension, corresponding to a dose 1 to 25 times higher than the minimal lethal dose, is injected intraperitoneally. Immediately after infection, mice are treated orally with a single dose of KB-5246. The number of mice surviving at each dose is counted 7 days after infection. The 50% effective dose is calculated by the probit method[1].

References:

[1]. Kotera Y, et al. In vitro and in vivo antibacterial activities of KB-5246, a new tetracyclic quinolone. Antimicrob Agents Chemother. 1989 Nov;33(11):1896-900.

Chemical Properties of KB-5246

Cas No. 119474-55-4 SDF
Canonical SMILES [H]Cl.CN1CCN(C2=C(F)C=C3C4=C2OCC5=CSC(N45)=C(C(O)=O)C3=O)CC1
Formula C18H17ClFN3O4S M.Wt 425.86
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of KB-5246

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1 mg 5 mg 10 mg
1 mM 2.3482 mL 11.7409 mL 23.4819 mL
5 mM 469.6 μL 2.3482 mL 4.6964 mL
10 mM 234.8 μL 1.1741 mL 2.3482 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Review for KB-5246

Average Rating: 5 ★★★★★ (Based on Reviews and 24 reference(s) in Google Scholar.)

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