Fleroxacin

Modify Date: 2024-01-02 14:27:16

Fleroxacin structure	Common Name	Fleroxacin
	CAS Number	79660-72-3	Molecular Weight	369.338
	Density	1.4±0.1 g/cm3	Boiling Point	535.3±50.0 °C at 760 mmHg
	Molecular Formula	C₁₇H₁₈F₃N₃O₃	Melting Point	264-266°C
	MSDS	Chinese USA	Flash Point	277.6±30.1 °C

Use of Fleroxacin

Fleroxacin is a broad-spectrum antimicrobial fluoroquinolone.Target: AntibacterialFleroxacin (Ro 23-6240; AM-833) is a new trifluorinated quinolone exhibiting high activity against a broad spectrum of gram-negative and gram-positive bacteria. Fleroxacin is characterized pharmacokinetically by a long elimination half-life (9 to 10 h) and high concentrations in plasma (e.g., maximum concentration of 2.3 micrograms/ml after an oral dose of 200 mg) [1]. Fleroxacin is effective against Haemophilus ducreyi in vitro. Fleroxacin, 200 or 400 mg as a single oral dose, is efficacious therapy for microbiologically proven chancroid in patients who do not have concurrent HIV-1 infection. Among HIV-1-infected men, a single dose of 200 or 400 mg of fleroxacin is inadequate therapy for chancroid [2, 3].

Name	Fleroxacin
Synonym	More Synonyms

Description	Fleroxacin is a broad-spectrum antimicrobial fluoroquinolone.Target: AntibacterialFleroxacin (Ro 23-6240; AM-833) is a new trifluorinated quinolone exhibiting high activity against a broad spectrum of gram-negative and gram-positive bacteria. Fleroxacin is characterized pharmacokinetically by a long elimination half-life (9 to 10 h) and high concentrations in plasma (e.g., maximum concentration of 2.3 micrograms/ml after an oral dose of 200 mg) [1]. Fleroxacin is effective against Haemophilus ducreyi in vitro. Fleroxacin, 200 or 400 mg as a single oral dose, is efficacious therapy for microbiologically proven chancroid in patients who do not have concurrent HIV-1 infection. Among HIV-1-infected men, a single dose of 200 or 400 mg of fleroxacin is inadequate therapy for chancroid [2, 3].
Related Catalog	Signaling Pathways >> Anti-infection >> Bacterial Research Areas >> Infection
References	[1]. Weidekamm, E., et al., Single- and multiple-dose pharmacokinetics of fleroxacin, a trifluorinated quinolone, in humans. Antimicrob Agents Chemother, 1987. 31(12): p. 1909-14. [2]. MacDonald, K.S., et al., Evaluation of fleroxacin (RO 23-6240) as single-oral-dose therapy of culture-proven chancroid in Nairobi, Kenya. Antimicrob Agents Chemother, 1989. 33(5): p. 612-4. [3]. Rubinstein, E., History of quinolones and their side effects. Chemotherapy, 2001. 47 Suppl 3: p. 3-8; discussion 44-8.

Description

Related Catalog

Signaling Pathways >> Anti-infection >> Bacterial

Research Areas >> Infection

References

[1]. Weidekamm, E., et al., Single- and multiple-dose pharmacokinetics of fleroxacin, a trifluorinated quinolone, in humans. Antimicrob Agents Chemother, 1987. 31(12): p. 1909-14.

[2]. MacDonald, K.S., et al., Evaluation of fleroxacin (RO 23-6240) as single-oral-dose therapy of culture-proven chancroid in Nairobi, Kenya. Antimicrob Agents Chemother, 1989. 33(5): p. 612-4.

[3]. Rubinstein, E., History of quinolones and their side effects. Chemotherapy, 2001. 47 Suppl 3: p. 3-8; discussion 44-8.

Density	1.4±0.1 g/cm3
Boiling Point	535.3±50.0 °C at 760 mmHg
Melting Point	264-266°C
Molecular Formula	C₁₇H₁₈F₃N₃O₃
Molecular Weight	369.338
Flash Point	277.6±30.1 °C
Exact Mass	369.130035
PSA	65.78000
LogP	1.72
Vapour Pressure	0.0±1.5 mmHg at 25°C
Index of Refraction	1.568
Storage condition	2-8°C

Fleroxacin MSDS(Chinese)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VB1999050

CHEMICAL NAME :: 3-Quinolinecarboxylic acid, 1,4-dihydro-6,8-difluoro-1-(2-fluoroethyl)-7-(4-methy l-1- piperazinyl)-4-oxo-

CAS REGISTRY NUMBER :: 79660-72-3

LAST UPDATED :: 199612

DATA ITEMS CITED :: 16

MOLECULAR FORMULA :: C17-H18-F3-N3-O3

MOLECULAR WEIGHT :: 369.38

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 20405 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 21730 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Musculoskeletal - joints

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 109 gm/kg/13W-I

TOXIC EFFECTS :: Musculoskeletal - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 4550 mg/kg/13W-I

TOXIC EFFECTS :: Behavioral - food intake (animal) Musculoskeletal - joints Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 26 gm/kg

SEX/DURATION :: male 61 day(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1300 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion Reproductive - Specific Developmental Abnormalities - musculoskeletal system

MUTATION DATA

TYPE OF TEST :: DNA damage

TEST SYSTEM :: Bacteria - Bacillus subtilis

DOSE/DURATION :: 400 ng/disk

REFERENCE :: NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 38(Suppl 2),252,1990

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes	Xn
RIDADR	NONH for all modes of transport
RTECS	VB1999050
HS Code	2933990090

Precursor 0
DownStream 1
CAS#:82419-46-3 Desmethylofloxacin

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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Fleroxacin

6,8-difluoro-1-(2-fluoroethyl)-1,4-dihydro-4-oxo-7-(4-methyl-1-piperazinyl)-quinoline-3-carboxylic acid

MEGALONE

6,8-difluoro-1-(2-fluoro-ethyl)-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid

6,8-Difluoro-1-(2-fluoroethyl)-7-(4-methyl-1-piperazinyl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid

ro23-6240/000

3-Quinolinecarboxylic acid, 6,8-difluoro-1-(2-fluoroethyl)-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-

Megalocin

AM-833

Quinodis

3-quinolinecarboxylicacid,1,4-dihydro-6,8-difluoro-1-(2-fluoroethyl)-7-(4-met

hyl-1-piperazinyl)-4-oxo

MFCD00864880

6,8-difluoro-1-(2-fluoroethyl)-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid

6,8-Difluoro-1-(2-fluoroethyl)-7-(4-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

6,8-difluoro-1-(2-fluoroethyl)-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic acid

RO-23-6240

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: Fleroxacin
Price: ￥418.0/5g ￥1518.0/25g
Purity: 98.0%
Stocking Period: Inquiry
Contact: Liu jia

DC Chemicals Limited
China
Product Name: Fleroxacin (Quinodis)
Price: $250.0/100mg $500.0/250mg $1000.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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Fleroxacin

Use of Fleroxacin

Names

Fleroxacin Biological Activity

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MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

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Precursor & DownStream

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