Grepafloxacin (OPC-17116) hydrochloride is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin hydrochloride has high tissue penetration and a promising pharmacodynamic profile.
性状
Solid
IC50 & Target[1][2]
Quinolone
体外研究(In Vitro)
Grepafloxacin (OPC-17116; 0-1 mg/L; 14-21 d) hydrochloride has antibiotic activity with a MIC value of ≤ 0.006 mg/L for E. coli strain.Grepafloxacin (0-1 mg/L; 3 h) hydrochloride has antimicrobial activity against mycobacteria in macrophages with a MIC value of 0.5 mg/L for M. avium .Grepafloxacin hydrochloride exhibits potent in vitro antibacterial activity against Gram-positive bacteria such as Streptococcus pneumoniae and high in vivo efficacy on the experimental systemic infections caused by the Gram-positive and -negative bacteria tested. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Grepafloxacin (OPC-17116; 200 mg/kg; p.o.; Balb/c mice) hydrochloride displays good safety profile in terms of phototoxicity.
Grepafloxacin (25-200 mg/kg; p.o.; 5 days/week for 4 weeks; female C57BL6/J-Lyst bg-J/ mice/beige mice) hydrochloride has modest activities in both intranasal (IN) infection and intravenous (IV) Mycobacterium avium infection models. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Vacher S, et, al. Comparative antimycobacterial activities of ofloxacin, ciprofloxacin and grepafloxacin. J Antimicrob Chemother. 1999 Nov;44(5):647-52.[2]. Owen K. Comparative grepafloxacin phototoxicity in mouse skin. J Antimicrob Chemother. 1998 Aug;42(2):261-4.[3]. Cynamon MH, et, al. The activity of grep