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119914-60-2

119914-60-2 structure
119914-60-2 structure
  • Name: Grepafloxacin
  • Chemical Name: Grepafloxacin
  • CAS Number: 119914-60-2
  • Molecular Formula: C19H22FN3O3
  • Molecular Weight: 359.39500
  • Catalog: API Synthetic anti-infective drugs Quinolone
  • Create Date: 2018-04-19 08:00:00
  • Modify Date: 2024-01-02 22:35:42
  • 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].

Name Grepafloxacin
Synonyms 1-cyclopropyl-6-fluoro-1,4-dihydro-5-methyl-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
1-cyclopropyl-5-methyl-6-fluoro-7-(3-methylpiperazin-1-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid
1-Cyclopropyl-6-fluoro-7-(3-methyl-1-piperazinyl)-5-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid
MFCD00865116
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].
Related Catalog
In Vitro Grepafloxacin is a once-daily fluoroquinolone[2]. 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].
In Vivo Grepafloxacin (OPC-17116) (200 mg/kg; p.o.; Balb/c mice) displays good safety profile in terms of phototoxicity[2]. Grepafloxacin (p.o.; 25, 50, 100, and 200 mg/kg; 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].
References

[1]. Efthymiopoulos C. Pharmacokinetics of grepafloxacin. J Antimicrob Chemother. 1997;40 Suppl A:35-43.

[2]. Owen K. Comparative grepafloxacin phototoxicity in mouse skin. J Antimicrob Chemother. 1998;42(2):261-264.

[3]. Cynamon MH, et al. The activity of grepafloxacin in two murine models of Mycobacterium avium infection. J Infect Chemother. 2004;10(3):185-188.

[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.

Density 1.366
Boiling Point 610ºC at 760mmHg
Melting Point 189-192ºC
Molecular Formula C19H22FN3O3
Molecular Weight 359.39500
Flash Point 322.7ºC
Exact Mass 359.16500
PSA 74.57000
LogP 2.67400

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VB1993785
CHEMICAL NAME :
3-Quinolinecarboxylic acid, 1,4-dihydro-1-cyclopropyl-6-fluoro-5-methyl-7-(3-meth yl- 1-piperazinyl)-4-oxo-
CAS REGISTRY NUMBER :
119914-60-2
LAST UPDATED :
199606
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C19-H22-F-N3-O3
MOLECULAR WEIGHT :
359.44

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
78 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,4531,1994
Hazard Codes Xi
Precursor  2

DownStream  0