Garenoxacin (BMS284756) 是一种具有口服活性的喹诺酮类抗生素 (antibiotic)，对各种革兰氏阳性和革兰氏阴性细菌、厌氧菌和复养微生物具有广泛的活性。
| 生物活性 | Garenoxacin (BMS284756) is an orally activequinoloneantibioticand has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms[1]. |
| IC50& Target[2] | Quinolone | Gyrase 1.25 μg/mL (IC50) | TOPO IV 1.5-2.5 μg/mL (IC50) |
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体外研究
(In Vitro) | Garenoxacin (BMS284756) (0-8 days) inhibits mycoplasmas and ureaplasmas with MIC90s ≤0.25 μg/mL against tested strains[1].
Garenoxacin (48 h) inhibitsS. aureuswild type and mutants with MICs of 0.0128-4.0 μg/mL[2].
Garenoxacin inhibits topoisomerase IV and gyrase fromS. aureuswith 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 ofS. aureus[3].
Cell Viability Assay[1] | Cell Line: | M. pneumonia,M. fermentans,M. hominisandUreaplasmaspp. | | Concentration: | | | Incubation Time: | 24 h forUreaplasmaspp., 48 h forM. hominis, 4 to 8 days forM. pneumonia | | Result: | Showed inhibition with MIC90s of 0.031 μg/mL, ≤0.008 μg/mL, ≤0.008 μg/mL and 0.25 μg/mL againstM. pneumonia,M. fermentans,M. hominisandUreaplasmaspp. strains, respectively. |
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体内研究
(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 withS. 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 byS. pneumoniaeD-979 in BALB/c female mice[5].
| Animal Model: | Swiss mice withS. pneumoniainfection[4]. | | Dosage: | 12.5, 25 and 50 mg/kg | | Administration: | Subcutaneous injection, once | | Result: | Significantly improved the survival rate. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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