Grepafloxacin hydrochloride  (Synonyms: OPC-17116 hydrochloride; dl-Grepafloxacin hydrochloride)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

395.86

C₁₉H₂₃ClFN₃O₃

161967-81-3

Solid

Yellow to orange

O=C(C1=CN(C2CC2)C3=C(C(C)=C(F)C(N4CC(C)NCC4)=C3)C1=O)O.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Vacher S, et, al. Comparative antimycobacterial activities of ofloxacin, ciprofloxacin and grepafloxacin. J Antimicrob Chemother. 1999 Nov;44(5):647-52.  [Content Brief]

  [2]. Owen K. Comparative grepafloxacin phototoxicity in mouse skin. J Antimicrob Chemother. 1998 Aug;42(2):261-4.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]