Garenoxacin mesylate hydrate

Research use only, not for human use.

A quinolone antibiotic for the treatment of Gram-positive and Gram-negative bacterial infections.

A quinolone antibiotic for the treatment of Gram-positive and Gram-negative bacterial infections.Bacterial Infection Approved(In Vitro):Garenoxacin (BMS284756) (0-8 days) inhibits mycoplasmas and ureaplasmas with MIC90s ≤0.25 μg/mL against tested strains.Garenoxacin (48 h) inhibits S. aureus wild type and mutants with MICs of 0.0128-4.0 μg/mL.Garenoxacin inhibits topoisomerase IV and gyrase from S. aureus with IC50s of 1.25 to 2.5 and 1.25 μg/mL, respectively.Garenoxacin has a low propensity for selective enrichment of fluoroquinolone-resistant mutants among ciprofloxacin-susceptible isolates of S. aureus.(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.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.

Garenoxacin (BMS284756) (0-8 days) inhibits mycoplasmas and ureaplasmas with MIC90s ≤0.25 μg/mL against tested strains.Garenoxacin (48 h) inhibits S. aureus wild type and mutants with MICs of 0.0128-4.0 μg/mL. Garenoxacin inhibits topoisomerase IV and gyrase from S. aureus with IC50s of 1.25 to 2.5 and 1.25 μg/mL, respectively.Garenoxacin has a low propensity for selective enrichment of fluoroquinolone-resistant mutants among ciprofloxacin-susceptible isolates of S. aureus. Cell Viability Assay 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 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 (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.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. Animal Model:Swiss mice with S. pneumonia infection.Dosage:12.5, 25 and 50 mg/kg Administration:Subcutaneous injection, once Result:Significantly improved the survival rate.

Garenoxacin mesylate [USAN] | BMS-284756-01 | Garenoxacin mesylate

GPCR/G Protein

Antibacterial

Antibacterial

Infection

Bacterial Infection

223652-90-2

540.5336

C24H26F2N2O8S

>98% (HPLC)

DMSO: ≥ 30 mg/mL

C[C@@H]1c2ccc(cc2CN1)c3ccc4c(c3OC(F)F)n(cc(c4=O)C(=O)O)C5CC5.CS(=O)(=O)O.O

3-Quinolinecarboxylic acid, 1-cyclopropyl-8-(difluoromethoxy)-7-[(1R)-2,3-dihydro-1-methyl-1H-isoindol-5-yl]-1,4-dihydro-4-oxo-, methanesulfonate, hydrate (1:1:1)

(-20℃)

With Ice Pack

≥ 2 years