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Antibiotics - DNA Regulation / Transcription
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ALX-380-295 Revised 15-Apr-08
Norfloxacin
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SYNONYMS 1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid
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ALX-380-295-G001   1 g 20.00 USD Add To Cart
ALX-380-295-G005   5 g 50.00 USD Add To Cart
Product Specification
FORMULA: C16H18FN3O3
MW: 319.3
CAS NUMBER: 70458-96-7
MERCK INDEX: 14: 6700
RTECS: VB2005000
PURITY: ≥98% (Assay)
APPEARANCE: White to yellow crystalline solid.
SOLUBILITY: Slightly soluble in water, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Fluoroquinolone antibacterial agent. Inhibits bacterial DNA replication. Blocks DNA replication by interfering with an ATP-induced structural transition of DNA complexed with DNA gyrase (topoisomerase). Effective against Gram-negative bacteria; less effective against Gram-positive bacteria. Potentially anxiogenic.
Product Specific Literature References
Structure-activity relationships of antibacterial 6,7- and 7,8-disubstituted 1-alkyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids: H. Koga, et al.; J. Med. Chem. 23, 1358 (1980) Abstract
Comparative activities of AM-715 and pipemidic and nalidixic acids against experimentally induced systemic and urinary tract infections: K. Hirai, et al.; Antimicrob. Agents Chemother. 19, 188 (1981) Abstract; Full Text
In vitro activity of MK-0366 against clinical urinary pathogens including gentamicin-resistant Pseudomonas aeruginosa: J. Downs, et al.; Antimicrob. Agents Chemother. 21, 670 (1982) Abstract
Comparison of the antibacterial activity of norfloxacin (MK 0366, AM 715), a new organic acid, with that of other orally absorbed chemotherapeutic agents: H.H. Gadebusch, et al.; Infection 10, 41 (1982) Abstract
Treatment of penicillin-resistant Neisseria gonorrhoeae with oral norfloxacin: S.R. Crider, et al.; N. Engl. J. Med. 311, 137 (1984) Abstract
Norfloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use: B. Holmes, et al.; Drugs 30, 482 (1985) Abstract
Norfloxacin: clinical pharmacology and clinical use: R.C. Rowen, et al.; Pharmacotherapy 7, 92 (1987) Abstract
Pharmacokinetic-pharmacodynamic modeling of the electroencephalogram effect of norfloxacin in rats: M. Chenel, et al.; Antimicrob. Agents Chemother. 47, 1952 (2003) Abstract; Full Text
Norfloxacin-induced DNA gyrase cleavage complexes block Escherichia coli replication forks, causing double-stranded breaks in vivo: J.R. Pohlhaus & K.N. Kreuzer; Mol. Microbiol. 56, 1416 (2005) Abstract; Full Text
Anxiogenic potential of ciprofloxacin and norfloxacin in rats: S. Sen, et al.; Singapore Med. J. 48, 1028 (2007) Abstract; Full Text
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Further Categories Containing This Product:
Antibiotics - Topoisomerase Inhibitors • Antibiotics - DNA Replication Inhibitors
 
 
ALX-380-296 Revised 15-Apr-08
Norfloxacin nicotinate
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SYNONYMS 1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid nicotinate
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ALX-380-296-G001   1 g 20.00 USD Add To Cart
ALX-380-296-G005   5 g 50.00 USD Add To Cart
Product Specification
FORMULA: C16H18FN3O3 . C6H5NO2
MW: 319.3 . 123.1
CAS NUMBER: 11803-81-9
PURITY: ≥98% (Assay)
APPEARANCE: White to yellow crystalline solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Fluoroquinolone antibacterial agent. Derivative of norfloxacin (Prod. No. ALX-380-296) with dramatically improved water solubility. Instantly dissociates into norfloxacin and nicotinic acid in the body therefore acting as norfloxacin. Inhibits bacterial DNA replication by interfering with an ATP-induced structural transition of DNA complexed with DNA gyrase (topoisomerase). Effective against Gram-negative bacteria; less effective against Gram-positive bacteria.
Product Specific Literature References
Efficacy of norfloxacin nicotinate treatment of broiler breeders against Haemophilus paragallinarum: A. Lublin, et al.; Avian Dis. 37, 673 (1993) Abstract
Norfloxacin nicotinate in the treatment of Pseudomonas aeruginosa infection in the genital tract of a bull: S. Marcus, et al.; Vet. Res. Commun. 18, 331 (1994) Abstract
Tissue distribution and binding to plasma proteins of norfloxacin nicotinate after intramuscular administration in pigs: M. Shem-Tov, et al.; Zentralbl. Veterinarmed. B. 41, 257 (1994) Abstract
Clinical pharmacokinetic characterization of norfloxacin nicotinate in swine following systemic administration: M. Shem-Tov & G. Ziv; Zentralbl. Veterinarmed. B. 41, 60 (1994) Abstract
Effect of lactation on single-dose pharmacokinetics of norfloxacin nicotinate in ewes: S. Soback, et al.; Antimicrob. Agents Chemother. 38, 2336 (1994) Abstract; Full Text
Intravenous disposition kinetics, oral and intramuscular bioavailability and urinary excretion of norfloxacin nicotinate in donkeys: E. Lavy, et al.; J. Vet. Pharmacol. Ther. 18, 101 (1995) Abstract
Norfloxacin nicotinate pharmacokinetics in unweaned and weaned calves: M. Gips & S. Soback; J. Vet. Pharmacol. Ther. 19, 130 (1996) Abstract
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Antibiotics - Topoisomerase Inhibitors • Antibiotics - DNA Replication Inhibitors
 
 
ALX-380-297 Revised 07-Aug-08
Ofloxacin
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SYNONYMS 9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazin-6-carboxylic acid
DL 8280
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ALX-380-297-G005   5 g 45.00 USD Add To Cart
Product Specification
FORMULA: C18H20FN3O4
MW: 361.4
CAS NUMBER: 82419-36-1
MERCK INDEX: 14: 6771
RTECS: UU8815500
PURITY: ≥98% (Assay)
APPEARANCE: White to yellow crystalline solid.
SOLUBILITY: Slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Fluoroquinolone with broad-spectrum antibacterial activity against most Gram-negative and Gram-positive bacteria. Effective against Mycobacterium tuberculosis.
Product Specific Literature References
In vitro and in vivo activity of DL-8280, a new oxazine derivative: K. Sato, et al.; Antimicrob. Agents Chemother. 22, 548 (1982) Abstract; Full Text
Comparison of the antibacterial in vitro and in vivo activity of ofloxacin (HOE 280 DL 8280) and nalidixic acid analogues: G. Seibert, et al.; Eur. J. Clin. Microbiol. 2, 548 (1983) Abstract
A new synthesis of 7H-pyrido[1,2,3-de][1,4]benzoxazine derivatives including an antibacterial agent, ofloxacin: H. Egawa, et al.; Chem. Pharm. Bull. 34, 4098 (1986) Abstract
Synthesis and antibacterial activities of optically active ofloxacin and its fluoromethyl derivative: S. Atarashi, et al.; Chem. Pharm. Bull. 35, 1896 (1987) Abstract
Ofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use: J.P. Monk & D.M. Campoli-Richards; Drugs 33, 346 (1987) Abstract
Mechanism of differential activities of ofloxacin enantiomers: I. Morrissey, et al.; Antimicrob. Agents Chemother. 40, 1775 (1996) Abstract; Full Text
Mechanism of fluoroquinolone action: K. Drlica; Curr. Opin. Microbiol. 2, 504 (1999) Abstract
Ofloxacin-like antibiotics inhibit pneumococcal cell wall-degrading virulence factors: C. Fernandez-Tornero, et al.; J. Biol. Chem. 280, 19948 (2005) Abstract; Full Text
Emergence of ofloxacin resistance in Mycobacterium tuberculosis clinical isolates from China as determined by gyrA mutation analysis using denaturing high-pressure liquid chromatography and DNA sequencing: R. Shi, et al.; J. Clin. Microbiol. 44, 4566 (2006) Abstract; Full Text
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy: R.K. Shandil, et al.; Antimicrob. Agents Chemother. 51, 576 (2007) Abstract; Full Text
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Further Categories Containing This Product:
Antibiotics - Topoisomerase Inhibitors • Antibiotics - DNA Replication Inhibitors
 
 
ALX-380-298 Revised 15-Apr-08
Pefloxacin . mesylate . dihydrate
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SYNONYMS 1-Ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid . monomethanesulfonate . dihydrate
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ALX-380-298-G005   5 g 30.00 USD Add To Cart
Product Specification
FORMULA: C17H20FN3O3 . CH4O3S . 2H2O
MW: 333.4 . 96.1 . 36.0
CAS NUMBER: 149676-40-4
MERCK INDEX: 14: 7066
RTECS: VB2002200
PURITY: ≥98%
APPEARANCE: White to yellow crystalline solid.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Fluoroquinolone antibacterial agent. Analog of norfloxacin (Prod. No. ALX-380-295). Prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse). Highly effective against Staphylococcus aureus, E. coli, other enterobacteria and Pseudomonas aeruginosa. Excellent effcectivity against Gram-negative bacteria, also effective against Gram-positive bacteria.
Product Specific Literature References
Absorption, distribution, metabolic fate, and elimination of pefloxacin mesylate in mice, rats, dogs, monkeys, and humans: G. Montay, et al.; Antimicrob. Agents Chemother. 25, 463 (1984) Abstract; Full Text
Activity of pefloxacin and thirteen other antimicrobial agents in vitro against isolates from hospital and genitourinary infections: B.M. Jones, et al.; J. Antimicrob. Chemother. 17, 739 (1986) Abstract
In vitro activity of pefloxacin against gram-negative and gram-positive bacteria in comparison with other antibiotics: E. Debbia, et al.; Chemioterapia 6, 319 (1987) Abstract
Studies on prodrugs. 7. Synthesis and antimicrobial activity of 3-formylquinolone derivatives: H. Kondo, et al.; J. Med. Chem. 31, 221 (1988) Abstract
In vitro effects of ciprofloxacin and pefloxacin on growth of normal human hematopoietic progenitor cells and on leukemic cell lines: E. Somekh, et al.; J. Pharmacol. Exp. Ther. 248, 415 (1989) Abstract
Binding interactions of pefloxacin mesylate with bovine lactoferrin and human serum albumin: J.C. Fan, et al.; J. Zhejiang Univ. Sci. B. 7, 452 (2006) Abstract; Full Text
Spectrophotometric determination of pefloxacin mesylate in pharmaceuticals: K. Basavaiah, et al.; Acta Pharm. 57, 221 (2007) Abstract
Further Categories Containing This Product:
Antibiotics - Topoisomerase Inhibitors • Antibiotics - DNA Replication Inhibitors
 
 
ALX-380-299 Revised 29-Jul-08
Prulifloxacin
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SYNONYMS 6-Fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
NM441
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ALX-380-299-M250   250 mg 90.00 USD Add To Cart
ALX-380-299-G001   1 g 270.00 USD Add To Cart
Product Specification
FORMULA: C21H20FN3O6S
MW: 461.5
CAS NUMBER: 123447-62-1
MERCK INDEX: 14: 7908
PURITY: ≥98% (Assay)
APPEARANCE: White to yellow crystalline solid.
SOLUBILITY: Slightly soluble in dimethyl formamide, 0.1M NaOH or glacial acetic acid; insoluble in water or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Fluoroquinolone with broad spectrum antibacterial activity against Gram-positive and Gram-negative bacteria.
Product Specific Literature References
In vivo evaluation of NM441, a new thiazeto-quinoline derivative: M. Ozaki, et al.; Antimicrob. Agents Chemother. 35, 2496 (1991) Abstract; Full Text
Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids: J. Segawa, et al.; J. Med. Chem. 35, 4727 (1992) Abstract
Pharmacokinetics and safety of NM441, a new quinolone, in healthy male volunteers: M. Nakashima, et al.; J. Clin. Pharmacol. 34, 930 (1994) Abstract
Randomized, double-blind study of prulifloxacin versus ciprofloxacin in patients with acute exacerbations of chronic bronchitis: C. Grassi, et al.; Respiration 69, 217 (2002) Abstract; Full Text
Pharmacologic characteristics of prulifloxacin: M.G. Matera; Pulm. Pharmacol. Ther. 19, 20 (2006) Abstract
Prulifloxacin: a new fluoroquinolone for the treatment of acute exacerbation of chronic bronchitis: M. Cazzola, et al.; Pulm. Pharmacol. Ther. 19, 30 (2006) Abstract
Prulifloxacin: a new antibacterial fluoroquinolone: G. Prats, et al.; Expert. Rev. Anti. Infect. Ther. 4, 27 (2006), (Review) Abstract
Further Categories Containing This Product:
Antibiotics - Topoisomerase Inhibitors • Antibiotics - DNA Replication Inhibitors
 
 
ALX-380-300 Revised 04-Aug-08
Rufloxacin . hydrochloride
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SYNONYMS 6-Fluoro-2,3-dihydro-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzothiazine-6-carboxylic acid . hydrochloride
MF-934 . hydrochloride
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ALX-380-300-M050   50 mg 50.00 USD Add To Cart
ALX-380-300-M250   250 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C17H18FN3O3S . HCl
MW: 363.4 . 36.5
CAS NUMBER: 106017-08-7
MERCK INDEX: 14: 8294
PURITY: ≥98% (Assay)
APPEARANCE: Off-white to light green crystalline solid.
SOLUBILITY: Sparingly soluble in water; very slightly soluble in methanol; almost insoluble in chloroform or acetic acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by IR.

Product Description
Fluoroquinolone antibacterial agent. Structurally similar to ofloxacin (Prod. No. ALX-380-297). Specific inhibitor of bacterial DNA gyrase (topoisomerase). Inhibits B-cell differentiation. Shows photosensitizing effects.
Product Specific Literature References
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids: V. Cecchetti, et al.; J. Med. Chem. 30, 465 (1987) Abstract
The in-vitro activity of two new quinolones: rufloxacin and MF 961: R. Wise, et al.; J. Antimicrob. Chemother. 29, 649 (1992) Abstract
Effect of rufloxacin on in-vitro proliferation and differentiation of human mononuclear cells: S. Gollapudi, et al.; J. Antimicrob. Chemother. 29, 669 (1992) Abstract
Multiple-dose pharmacokinetics and safety of rufloxacin in normal volunteers: J.C. Kisicki, et al.; Antimicrob. Agents Chemother. 36, 1296 (1992) Abstract; Full Text
Double-blind, comparative study of rufloxacin once daily versus amoxicillin three times a day in treatment of outpatients with exacerbations of chronic bronchitis: W. Klietmann, et al.; Antimicrob. Agents Chemother. 37, 2298 (1993) Abstract; Full Text
Rufloxacin once daily versus ofloxacin twice daily for treatment of complicated cystitis and upper urinary tract infections. Italian Multicentre UTI Rufloxacin Group: R. Mattina, et al.; Infection 21, 106 (1993) Abstract
Comparison of the mechanism of action and resistance of two new fluoroquinolones, rufloxacin and MF961 with those of ofloxacin and fleroxacin in gram-negative and gram-positive bacteria: L.J. Piddock, et al.; J. Antimicrob. Chemother. 31, 855 (1993) Abstract
Molecular mechanisms of photosensitization induced by drugs. XII. Photochemistry and photosensitization of rufloxacin: an unusual photodegradation path for the antibacterials containing a fluoroquinolone-like chromophore: G. Condorelli, et al.; Photochem. Photobiol. 70, 280 (1999) Abstract
Penetration of rufloxacin into the cerebrospinal fluid in patients with inflamed and uninflamed meninges: M.V. Moretti, et al.; Antimicrob. Agents Chemother. 44, 73 (2000) Abstract; Full Text
Rufloxacin-induced photosensitization in yeast: A. Catalfo, et al.; Photochem. Photobiol. Sci. 6, 181 (2007) Abstract
Further Categories Containing This Product:
Antibiotics - Topoisomerase Inhibitors • Antibiotics - DNA Replication Inhibitors
 
 
ALX-380-301 Revised 04-Aug-08
Sarafloxacin . hydrochloride
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SYNONYMS 6-Fluoro-1-(4-fluorophenyl)-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid .
hydrochloride
A-56620
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ALX-380-301-G005   5 g 50.00 USD Add To Cart
ALX-380-301-G025   25 g 150.00 USD Add To Cart
Product Specification
FORMULA: C20H17F2N3O3 . HCl
MW: 385.4 . 36.5
CAS NUMBER: 91296-87-6
MERCK INDEX: 14: 8370
PURITY: ≥98% (Assay)
APPEARANCE: White to yellow crystalline solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by IR.

Product Description
Fluoroquinolone antibacterial agent. Inhibits bacterial DNA gyrase (topoisomerase). Effective against Mycobacterium tuberculosis.
Product Specific Literature References
Synthesis and structure-activity relationships of novel arylfluoroquinolone antibacterial agents: D.T. Chu, et al.; J. Med. Chem. 28, 1558 (1985) Abstract
In vivo evaluation of A-56619 (difloxacin) and A-56620: new aryl-fluoroquinolones: P.B. Fernandes, et al.; Antimicrob. Agents Chemother. 29, 201 (1986) Abstract; Full Text
In-vitro activity of six fluorinated quinolones against Mycobacterium tuberculosis: O.G. Berlin, et al.; J. Antimicrob. Chemother. 19, 611 (1987) Abstract
In vitro activities of A-56619 (difloxacin) and A-56620, two aryl fluoroquinolones: A. Digranes & W.L. Dibb; Chemotherapy 34, 298 (1988) Abstract
Determination of temafloxacin, sarafloxacin, and difloxacin in bulk drug and dosage forms by high-performance liquid chromatography: J.F. Bauer, et al.; Pharm. Res. 7, 1177 (1990) Abstract
Further Categories Containing This Product:
Antibiotics - Topoisomerase Inhibitors • Antibiotics - DNA Replication Inhibitors
 
 
ALX-380-302 Revised 15-Aug-08
Sparfloxacin
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SYNONYMS rel-5-Amino-1-cyclopropyl-7-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
AT-4140
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ALX-380-302-G001   1 g 70.00 USD Add To Cart
ALX-380-302-G005   5 g 280.00 USD Add To Cart
Product Specification
FORMULA: C19H22F2N4O3
MW: 392.4
CAS NUMBER: 110871-86-8
MERCK INDEX: 14: 8735
RTECS: VB1986500
PURITY: ≥98% (Assay)
APPEARANCE: White to yellow crystalline solid.
SOLUBILITY: Soluble in 100% ethanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: IRRITANT.

Product Description
Fluoroquinolone with broad spectrum antibacterial activity against Gram-positive and Gram-negative bacteria. Inhibits bacterial DNA gyrase (topoisomerase). Effective against Mycobacterium tuberculosis. Shows photosensitizing effects.
Product Specific Literature References
In vitro and in vivo antibacterial activities of AT-4140, a new broad-spectrum quinolone: S. Nakamura, et al.; Antimicrob. Agents Chemother. 33, 1167 (1989) Abstract; Full Text
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency: T. Miyamoto, et al.; J. Med. Chem. 33, 1645 (1990) Abstract
Pharmacokinetics of a novel quinolone, AT-4140, in animals: S. Nakamura, et al.; Antimicrob. Agents Chemother. 34, 89 (1990) Abstract; Full Text
Mechanism of action of sparfloxacin against and mechanism of resistance in gram-negative and gram-positive bacteria: L.J. Piddock & M. Zhu; Antimicrob. Agents Chemother. 35, 2423 (1991) Abstract; Full Text
The link between sunshine and phototoxicity of sparfloxacin: C. Pierfitte, et al.; Br. J. Clin. Pharmacol. 49, 609 (2000) Abstract; Full Text
Sparfloxacin: a review: J.J. Schentag; Clin. Ther. 22, 372 (2000), (Review) Abstract
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy: R.K. Shandil, et al.; Antimicrob. Agents Chemother. 51, 576 (2007) Abstract; Full Text
Further Categories Containing This Product:
Antibiotics - Topoisomerase Inhibitors • Antibiotics - DNA Replication Inhibitors
 
 
ALX-380-303 Revised 15-Apr-08
Tosufloxacin . tosylate
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SYNONYMS 7-(3-Amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid . tosylate
A-64730
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ALX-380-303-M250   250 mg 90.00 USD Add To Cart
ALX-380-303-G001   1 g 270.00 USD