Garenoxacin
Based on 1 Customer Validation
Garenoxacin (BMS284756) is an orally active quinolone antibiotic and has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms.
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- Purity: 98.62%
- CAS No.: 194804-75-6
- 화학식: C23H20F2N2O4
- 분자량:426.41
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
Quinolone |
Gyrase 1.25 μg/mL (IC50) |
TOPO IV 1.5-2.5 μg/mL (IC50) |
Garenoxacin (BMS284756) (0-8 days) inhibits mycoplasmas and ureaplasmas with MIC90s ≤0.25 μg/mL against tested strains[1].
Garenoxacin (48 h) inhibits S. aureus wild type and mutants with MICs of 0.0128-4.0 μg/mL[2].
Garenoxacin inhibits topoisomerase IV and gyrase from S. aureus with IC50s of 1.25 to 2.5 and 1.25 μg/mL, respectively[2].
Garenoxacin has a low propensity for selective enrichment of fluoroquinolone-resistant mutants among ciprofloxacin-susceptible isolates of S. aureus[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:M. pneumonia, M. fermentans, M. hominis and Ureaplasma spp.
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Concentration:
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Incubation Time:24 h for Ureaplasma spp., 48 h for M. hominis, 4 to 8 days for M. pneumonia
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Result:Showed inhibition with MIC90s of 0.031 μg/mL, ≤0.008 μg/mL, ≤0.008 μg/mL and 0.25 μg/mL against M. pneumonia, M. fermentans, M. hominis and Ureaplasma spp. strains, respectively.
Garenoxacin (10 and 30 mg/kg; p.o.; once) reduces the viable cell counts in the lungs and significantly prolongs survival on experimental secondary pneumococcal pneumonia caused by S. pneumoniae D-979 in BALB/c female mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss mice with S. pneumonia infection[4].
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Dosage:12.5, 25 and 50 mg/kg
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Administration:Subcutaneous injection, once
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Result:Significantly improved the survival rate.
Chemical Information
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CAS No. 194804-75-6
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Appearance Solid
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분자량 426.41
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화학식 C23H20F2N2O4
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Color White to off-white
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SMILES
O=C(C1=CN(C2CC2)C3=C(C=CC(C4=CC5=C([C@@H](C)NC5)C=C4)=C3OC(F)F)C1=O)O
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Synonyms
BMS284756
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 5 mg/mL (11.73 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Waites KB, et al. In vitro susceptibilities to and bactericidal activities of garenoxacin (BMS-284756) and other antimicrobial agents against human mycoplasmas and ureaplasmas. Antimicrob Agents Chemother. 2003 Jan;47(1):161-5. [Content Brief]
[2]. Ince D, et al. Dual targeting of DNA gyrase and topoisomerase IV: target interactions of garenoxacin (BMS-284756, T-3811ME), a new desfluoroquinolone. Antimicrob Agents Chemother. 2002 Nov;46(11):3370-80. [Content Brief]
[3]. Zhao X, et al. Mutant prevention concentration of garenoxacin (BMS-284756) for ciprofloxacin-susceptible or -resistant Staphylococcus aureus. Antimicrob Agents Chemother. 2003 Mar;47(3):1023-7. [Content Brief]
[4]. Azoulay-Dupuis E, et al. Activities of garenoxacin against quinolone-resistant Streptococcus pneumoniae strains in vitro and in a mouse pneumonia model. Antimicrob Agents Chemother. 2004 Mar;48(3):765-73. [Content Brief]
[5]. Fukuda Y, et al. Therapeutic effects of garenoxacin in murine experimental secondary pneumonia by Streptococcus pneumoniae after influenza virus infection. Diagn Microbiol Infect Dis. 2014 Feb;78(2):168-71. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3452 mL | 11.7258 mL | 23.4516 mL | 58.6290 mL |
| 5 mM | 0.4690 mL | 2.3452 mL | 4.6903 mL | 11.7258 mL | |
| 10 mM | 0.2345 mL | 1.1726 mL | 2.3452 mL | 5.8629 mL |