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Purity: ≥98%
BAY-Y 3118 is novel and potent chlorofluoroquinolone derivative with antimicrobial activity against Haemophilhs influenzae, Moraxela catarrhalis, Acinetobacter baumannii, Xanthomonas maltophiia, gram-positive cocci, and anaerobes; MICs for 50%o of the strains (MIC50s) and MIC90s are ≤0.015 and ≤0.015, ≤0.015 and ≤0.015, 0.03 and 2, 0.25 and 0.5, 0.06 and 1, and 0.12 and 0.25 μg/mL, respectively. The cellular concentration-to-extracellular concentration ratio of BAY-Y 3118 is higher than 6.3 at extracellular concentrations ranging from 2 to 100 mg/L. The uptake of BAY-Y 3118 is rapid, reversible and nonsaturable. The intracellular penetration of BAY-Y 3118 is significantly affected by environmental temperature and cell viability. BAY-Y 3118 reaches high intracellular concentrations within human polymorphonuclear leukocytes (PMNs) and remains active intracellularly. All strains of L. monocytogenes and other Listeria spp. are highly susceptible; the MICs for these organisms ranges from 0.062 to 0.25 μg/mL. BAY-Y 3118 is rapidly bactericidal in vitro, with a postantibiotic effect occurring for 3 h after removal of the antibiotic. L. monocytogenes is eliminated from infected L929 cells treated with BAY-Y 3118, suggesting a bactericidal effect on the listeriae in these cells.
| ln Vitro |
Acinetobacter baumannii, Xanthomonas maltomonas, Haemophilus influenzae, Moraxella catarrhalis, Gram-positive cocci, and anaerobic bacteria are among the strains against which BAY-Y 3118 is effective; its MIC (MIC50) and MIC90, which represent 50% of the strains, are ≤0.015 and ≤0.015, ≤0.015 and ≤0.015, 0.03 and 2, 0.25 and 0.5, 0.06 and 1, 0.12 and 0.25 μg/mL[1]. At extracellular concentrations ranging from 2 to 100 mg/L, BAY-Y 3118's cellular to extracellular concentration ratio was more than 6.3. BAY-Y 3118 is absorbed quickly, reversibly, and unsaturatedly. Cell viability and ambient temperature have a major impact on BAY-Y 3118's capacity to penetrate cells inside of them. Human polymorphonuclear leukocytes (PMN) contain substantial intracellular quantities of BAY-Y 3118, which is still active within the cells [2]. All strains of Listeria spp., including Listeria monocytogenes. Extremely sensitive; these organisms have a MIC range of 0.062 to 0.25 μg/mL. In vitro, BAY-Y 3118 exhibits a fast bactericidal action, exhibiting post-antibiotic effects within 3 hours of antibiotic withdrawal. Infected L929 cells treated with BAY-Y 3118 showed the elimination of Listeria monocytogenes, suggesting that the compound had a bactericidal effect on Listeria in these cells [3].
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| ln Vivo |
Treating immunocompetent mice with 4 mg every 12 hours resulted in a quick recovery. Simultaneously, the mouse serum's levels of gamma interferon and interleukin-6 dropped quickly. Compared to treating immunocompetent mice with 2 mg of ampicillin every 12 hours, treating them with 2 mg of BAY-Y 3118 every 12 hours produced a larger initial reduction in organ Listeria counts. Listeria monocytogenes in the liver and spleen of chronically infected nude mice are totally eradicated by BAY-Y 3118 [3].
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| References |
[1]. Fass RJ, et al. In vitro activity of Bay y 3118, a new quinolone. Antimicrob Agents Chemother. 1993 Nov;37(11):2348-57.
[2]. García I, et al. Intracellular penetration and activity of BAY Y 3118 in human polymorphonuclear leukocytes. Antimicrob Agents Chemother. 1994 Oct;38(10):2426-9. [3]. Nichterlein T, et al. Bay Y 3118, a new quinolone derivative, rapidly eradicates Listeria monocytogenes from infected mice and L929 cells. Antimicrob Agents Chemother. 1994 Jul;38(7):1501-6 |
| Molecular Formula |
C20H21CLFN3O3
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| Molecular Weight |
405.850447416306
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| CAS # |
151213-16-0
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| Related CAS # |
(R,R)-BAY-Y 3118;151213-22-8
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| SMILES |
O=C(C1=CN(C2CC2)C3=C(C=C(F)C(N(C4)C[C@]5([H])[C@@]4([H])CCCN5)=C3Cl)C1=O)O
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| Synonyms |
BAY-Y 3118; BAY-Y-3118; BAY Y 3118;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~82.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.16 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4640 mL | 12.3198 mL | 24.6396 mL | |
| 5 mM | 0.4928 mL | 2.4640 mL | 4.9279 mL | |
| 10 mM | 0.2464 mL | 1.2320 mL | 2.4640 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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