Garenoxacin (BMS284756) Mesylate hydrate 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) Mesylate hydrate 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 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(185.00 mM;Need ultrasonic) H2O : 12.5 mg/mL(23.13 mM;Need ultrasonic) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.63 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.63 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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