| Bioactivity | 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[1][2][3][4]. |
| Invitro | 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[1].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[1].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[4]. |
| In Vivo | Grepafloxacin (OPC-17116; 200 mg/kg; p.o.; Balb/c mice) hydrochloride displays good safety profile in terms of phototoxicity[2]. 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[3]. |
| Name | Grepafloxacin hydrochloride |
| CAS | 161967-81-3 |
| Formula | C19H23ClFN3O3 |
| Molar Mass | 395.86 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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 grepafloxacin in two murine models of Mycobacterium avium infection. J Infect Chemother. 2004 Jun;10(3):185-8. [4]. Miyamoto H, et al. Synthesis and biological properties of substituted 1,4-dihydro-5-methyl-4-oxo-3-quinolinecarboxylic acids. Bioorg Med Chem. 1995;3(12):1699-1706. |
Grepafloxacin hydrochloride
CAS: 161967-81-3 F: C19H23ClFN3O3 W: 395.86
Grepafloxacin (OPC-17116) hydrochloride is an oral actively fluoroquinolone antibiotic with potent activity against comm
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