Garenoxacin 是一种新型的口服 des-fluoro(6) 喹诺酮,有抗菌活性,可抑制呼吸道病原体。
产品描述
Garenoxacin is a novel oral des-fluoro(6) quinolone for the treatment of Gram-positive and Gram-negative bacterial infections.
体内活性
The mean maximum plasma concentration (Cmax ) was 3.00 ± 1.12 μg/mL, time to maximum plasma concentration (Tmax ) was 3.0 ± 2.0 hours, and area under the curve for 24 hours (AUC0-24 ) was 40.7 ± 16.7 μg·h/mL. The half-life (T1/2 ) of GRNX could not be calculated because plasma concentrations remained high 24 hours after administration. Cmax was strongly associated with the GRNX dose per kilogram body weight (r = 0.85, P = 0.03).Clinically, fever resolved within 3 days of GRNX administration and C-reactive protein levels returned to normal 14 days after administration. One patient experienced temporary increases in serum transaminase levels[1].
动物实验
Six male patients with infections who were undergoing MH received 200 mg GRNX once daily. Blood samples were taken before and at 1, 2, 4, 6, 12, and 24 hours after GRNX administration. Plasma GRNX concentrations were measured using high-performance liquid chromatography[1].
Cas No.
194804-75-6
分子式
C23H20F2N2O4
分子量
426.42
别名
加雷沙星;BMS284756;Garenoxacin
储存和溶解度
DMSO:2 mg/mL (4.69 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years