[CAS NO. 223652-90-2] GarenoxacinMesylatehydrate
PRODUCTS SPECIFICATIONS [223652-90-2]
DESCRIPTION [223652-90-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 540.53 |
| Molecular Formula | C24H26F2N2O8S |
| 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.CS(=O)(O)=O.O |
Summary
Garenoxacin (BMS284756) Mesylate hydrate 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 [1] .
IC50 & Target
|
Quinolone
|
Gyrase 1.25 μg/mL (IC 50 ) |
TOPO IV 1.5-2.5 μg/mL (IC 50 ) |
In Vitro
Garenoxacin (BMS284756) (0-8 days) inhibits mycoplasmas and ureaplasmas with MIC
90
s ≤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 IC
50
s 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | M. pneumonia , M. fermentans , M. hominis and Ureaplasma spp. |
| Concentration: | |
| Incubation Time: | 24 h for Ureaplasma spp., 48 h for M. hominis , 4 to 8 days for M. pneumonia |
| Result: | Showed inhibition with MIC 90 s 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. |
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. pneumonia
infection
[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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL ( 185.00 mM ; Need ultrasonic)
H 2 O : 12.5 mg/mL ( 23.13 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8500 mL | 9.2502 mL | 18.5004 mL |
| 5 mM | 0.3700 mL | 1.8500 mL | 3.7001 mL |
| 10 mM | 0.1850 mL | 0.9250 mL | 1.8500 mL |
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.
- [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.
- [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.
- [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.
- [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.
Synonyms
