| Identification | Back Directory | [Name]
Garenoxacin | [CAS]
223652-90-2 | [Synonyms]
Garenoxacin mesylate [USAN]
BMS284756 (Mesylate hydrate)
Garenoxacin mesylate hydrate
Garenoxacin mesylate monohydrate >=98% (HPLC)
1-cyclopropyl-8-(difluoromethoxy)-4-keto-7-[(1R)-1-methylisoindolin-5-yl]quinoline-3-carboxylic acid
1-cyclopropyl-8-(difluoromethoxy)-7-[(1R)-1-methyl-2,3-dihydro-1H-isoindol-5-yl]-4-oxoquinoline-3-carboxylicacid,methanesulfonicacid,hydrate
1-Cyclopropyl-8-(difluoromethoxy)-7-[(1R)-2,3-dihydro-1-methyl-1H-isoindol-5-yl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid methanesulfonate hydrate
(R)-1-cyclopropyl-8-(difluoromethoxy)-7-(1-methylisoindolin-5-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid compound with methanesulfonic acid (1:1) hydrate
Garenoxacin mesylate hydrate
1-Cyclopropyl-8-(difluoromethoxy)-7-[(1R)-2,3-dihydro-1-methyl-1H-isoindol-5-yl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid methanesulfonate hydrate | [Molecular Formula]
C23H20F2N2O4.CH4O3S.H2O | [MDL Number]
MFCD12031996 | [MOL File]
223652-90-2.mol | [Molecular Weight]
540.53 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
DMSO:100.0(Max Conc. mg/mL);185.0(Max Conc. mM)
Water:12.5(Max Conc. mg/mL);23.13(Max Conc. mM) | [form ]
powder | [color ]
white to beige | [Water Solubility ]
H2O: 10mg/mL, clear (warmed) | [InChIKey]
IGTHEWGRXUAFKF-NVJADKKVSA-N | [SMILES]
OC(C1=CN(C2CC2)C3=C(OC(F)F)C(C4=CC(CN[C@@H]5C)=C5C=C4)=CC=C3C1=O)=O.CS(=O)(O)=O.[H]O[H] |
| Hazard Information | Back Directory | [Uses]
Antibacterial agent. | [Biological Activity]
Garenoxacin is a broad spectrum fluoroquinolone antibiotic suitable for treatment of gram-positive and gram-negative bacterial infections. Garenoxacin has a low mutant prevention concentration and a narrow mutant selection window. Data shows th at garenoxacin has anti-inflammatory properties. It significantly alleviates LPS-induced IL-8 production through the negative regulation of the ERK1/2 pathway both in the human airway epithelial cell line A549 and the monocyte cell line THP-1. | [in vivo]
Garenoxacin (12.5-50 mg/kg; s.c.; once) is highly effective against the wild-type strain and mutants harboring a single mutation in a mouse pneumonia model with S. pneumoniainfection[4].
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]. | Animal Model: | Swiss mice with S. pneumonia infection[4]. | | Dosage: | 12.5, 25 and 50 mg/kg | | Administration: | Subcutaneous injection, once | | Result: | Significantly improved the survival rate. |
| [IC 50]
Quinolone; Gyrase: 1.25 μg/mL (IC50); TOPO IV: 1.5-2.5 μg/mL (IC50) |
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