1. Grepafloxacin

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

Cat. No.: HY-A0147
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Grepafloxacin (OPC-17116) is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile.

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Grepafloxacin Chemical Structure

Grepafloxacin Chemical Structure

CAS No. : 119914-60-2

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Description

Grepafloxacin (OPC-17116) is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile[1][2][3].

In Vitro

Grepafloxacin (OPC-17116; 0-1 mg/L; 14-21 d) has antibiotic activity with a MIC value of ≤ 0.006 mg/L for E. coli strain[1].
Grepafloxacin (0-1 mg/L; 3 h) has antimicrobial activity against mycobacteria in macrophages with a MIC value of 0.5 mg/L for M. 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].

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

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 avium infection models[3].

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

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 with mycobacterium avium infection[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.
Molecular Weight

359.39

Formula

C19H22FN3O3

CAS No.
SMILES

O=C(C1=CN(C2CC2)C3=C(C(C)=C(F)C(N4CC(C)NCC4)=C3)C1=O)O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Grepafloxacin
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HY-A0147
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