Grepafloxacin (OPC-17116) 是一种口服活性氟喹诺酮类抗生素 (antibiotic)，对包括肺炎链球菌在内的社区获得性呼吸道病原体具有有效活性。Grepafloxacin 具有较高的组织渗透性和良好的药效学特性。
| 生物活性 | Grepafloxacin (OPC-17116) is an oral actively fluoroquinoloneantibioticwith potent activity against community-acquired respiratory pathogens includingStreptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile[1][2][3]. |
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体外研究
(In Vitro) | Grepafloxacin (OPC-17116; 0-1 mg/L; 14-21 d) has antibiotic activity with a MIC value of ≤ 0.006 mg/L forE. colistrain[1].
Grepafloxacin (0-1 mg/L; 3 h) has antimicrobial activity against mycobacteria in macrophages with a MIC value of 0.5 mg/L forM. avium[1].
Grepafloxacin 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].
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体内研究
(In Vivo) | Grepafloxacin (OPC-17116; 200 mg/kg; p.o.; Balb/c mice) 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) has modest activities in both intranasal (IN) infection and intravenous (IV)Mycobacterium aviuminfection models[3].
| Animal Model: | Female Balb/c mice (5-6 weeks)[2] | | Dosage: | 200 mg/kg | | Administration: | Oral administration; once | | Result: | Had mild and short-lived erythema and no changed auricular thickness. |
| Animal Model: | Female C57BL6/J-Lyst bg-J/ mice/beige mice withmycobacterium aviuminfection[3] | | Dosage: | 25, 50, 100, and 200 mg/kg | | Administration: | Oral administration; 5 days/week for 4 weeks | | Result: | Had bactericidal activity and limited the growth of the bacteria. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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