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Sparfloxacin

Sparfloxacin Struktur
110871-86-8
CAS-Nr.
110871-86-8
Englisch Name:
Sparfloxacin
Synonyma:
Parox;Zagam;ci978;Spara;at4140;Sparcin;RP-64206;CP 103826;PD 1315-1;Sparfloxacin
CBNumber:
CB7407291
Summenformel:
C19H22F2N4O3
Molgewicht:
392.4
MOL-Datei:
110871-86-8.mol

Sparfloxacin Eigenschaften

Schmelzpunkt:
265°C
Siedepunkt:
640℃
Dichte
1.436±0.06 g/cm3(Predicted)
Flammpunkt:
>110°(230°F)
storage temp. 
Keep in dark place,Inert atmosphere,2-8°C
L?slichkeit
DMF: 10 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.50 mg/ml
pka
pKa1 6.25, pKa2 9.30(at 25℃)
Aggregatzustand
powder
Farbe
white to light yellow
Wasserl?slichkeit
Soluble in DMSO at 9mg/ml. Sparingly soluble in water
BRN 
9170271
CAS Datenbank
110871-86-8(CAS DataBase Reference)
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Kennzeichnung gef?hrlicher Xi
R-S?tze: 36/37/38
S-S?tze: 26-36
WGK Germany  2
RTECS-Nr. VB1986500
HS Code  29339900
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H315 Verursacht Hautreizungen. Hautreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P302+P352, P321,P332+P313, P362
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
H335 Kann die Atemwege reizen. Spezifische Zielorgan-Toxizit?t (einmalige Exposition) Kategorie 3 (Atemwegsreizung) Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" />
Sicherheit
P261 Einatmen von Staub vermeiden.
P264 Nach Gebrauch gründlich waschen.
P264 Nach Gebrauch gründlich waschen.
P271 Nur im Freien oder in gut belüfteten R?umen verwenden.
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.
P302+P352 BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen.

Sparfloxacin Chemische Eigenschaften,Einsatz,Produktion Methoden

R-S?tze Betriebsanweisung:

R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.

S-S?tze Betriebsanweisung:

S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.

Beschreibung

Sparfloxacin is the most potent fluoroquinolone antibiotic introduced for the treatment of community acquired infections. It has superior and broad in vitro activity against members of family Enterobacferiaceae and anaerobic bacteria, some of which are resistant toβ-lactam antibiotics or to aminoglycosides. In patients with surgical infections, sparfloxacin shows excellent activity against resistant pathogens. It is effective in treating patients with bladder irritability and is reported to have potential in the treatment of leprosy and Mycobacterium tuberculosis in mice. Favorable pharmacokinetic properties, good intracellular penetration and a lack of transferable resistance have been reported.

Chemische Eigenschaften

Light yellow powder

Weltgesundheitsorganisation (WHO)

Sparfloxacin is a quinolone antimicrobial agent. See also under quinolone and fluoroquinolone antimicrobial agents.

Pharmazeutische Anwendungen

It is highly active against most aerobic Grampositive cocci and Gram-negative bacilli, including fastidious Gram-negative bacilli, Acinetobacter spp., Campylobacter spp. and Legionella spp. Ps. aeruginosa is weakly susceptible. Activity also extends to the genital mycoplasmas, M. tuberculosis and M. avium complex isolates. It is moderately active against some anaerobes (including the B. fragilis group); L. monocytogenes is resistant.
It is well absorbed, achieving a plasma concentration of 1–1.5 mg/L 4.5 h after a 400 mg oral dose. Absorption is decreased in the presence of antacids owing to the formation of chelates with metallic ions. Concentrations in many tissues, including lung, exceed those in plasma. The plasma half-life is 15–20 h. CSF penetration is limited. Around 5–10% of a dose is eliminated unchanged in the urine, with about 30% appearing as the glucuronide. Total clearance is 10–15 L/h. The plasma half-life increases only modestly in renal failure to 30–40 h. About 50–60% of the dose appears as unchanged drug in the feces, mainly as the glucuronide, accounting for 10–20% of the administered dose.
Adverse events are those common to fluoroquinolones, in particular gastrointestinal tract disturbances, CNS effects (mainly headache and insomnia) and rashes. Photosensitivity reactions have been observed in 2–11% of patients. It can prolong the QTc interval and cases of torsade de pointes have been reported. It does not potentiate the toxicity of theophylline.
It has been used for respiratory and other infections caused by susceptible bacteria, but use has been restricted in the USA and Europe because of phototoxicity and cardiotoxicity.

Clinical Use

Sparfloxacin, (cis)-5-amino-1-cyclopropyl-7-(3,5-dimethyl)-1-piperazinyl)-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylicacid, is a newer fluoroquinolone.
This compound exhibits higher potency against Grampositivebacteria, especially staphylococci and streptococci,than the fluoroquinolones currently marketed. It is also moreactive against chlamydia and the anaerobe Bacteroides fragilis.The activity of sparfloxacin against Gram-negative bacteriais also very impressive, and it compares favorably withciprofloxacin and ofloxacin in potency against Mycoplasmaspp., Legionella spp., Mycobacteria spp., and Listeria monocytogenes.Sparfloxacin has a long elimination half-life of18 hours, which permits once-a-day dosing for most indications.The drug is widely distributed into most fluidsand tissues. Effective concentrations of sparfloxacin areachieved for the treatment of skin and soft tissue infections,lower respiratory infections (including bronchitis and bacterialpneumonias), and pelvic inflammatory disease causedby gonorrhea and chlamydia. Sparfloxacin has also beenrecommended for the treatment of bacterial gastroenteritisand cholecystitis. The oral bioavailability of sparfloxacinis claimed to be good, and sufficient unchanged drug isexcreted to be effective for the treatment of urinary tract infections.Nearly 20% of an orally administered dose is excretedas an inactive glucuronide.

Sparfloxacin Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Sparfloxacin Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 370)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Hangzhou FandaChem Co.,Ltd.
+8615858145714
FandaChem@Gmail.com China 9080 55
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28172 58
Henan Xiangtong Chemical Co., Ltd.
86-371-61312303
info@hnxtchem.com CHINA 292 58
Hubei xin bonus chemical co. LTD
86-13657291602
linda@hubeijusheng.com CHINA 22963 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49374 58
career henan chemical co
+86-0371-86658258 +8613203830695
factory@coreychem.com China 29810 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 32161 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226
sales@hzclap.com CHINA 6312 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250
1026@dideu.com China 22787 58
AFINE CHEMICALS LIMITED
+86-0571-85134551
sales@afinechem.com China 15352 58

110871-86-8()Verwandte Suche:


  • Sparfloxacin Solution, 100ppm
  • Sparfloxacin solution,1000ppm
  • 5-Amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-(3α,5α-dimethyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic acid
  • 5-Amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-(3β,5β-dimethyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic acid
  • RP-64206
  • 5-Amino-1-cyclopropyl-7-(3,5-dimethyl-1-piperazinyl)-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
  • Sparfloxacin
  • Sparfloxacine
  • cis-5-AMino-1-cyclopropyl-7-(3,5-diMethyl-1-piperazinyl)-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic Acid
  • Sparcin
  • AT-4140,CI-978,PD 131501
  • rel-5-amino-1-cyclopropyl-7-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
  • (cis)-5-Amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-(3,5-dimethyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
  • PD-131501:Spara
  • 5-AMINO-1-CYCLOHEXYL-7-(CIS-3,5-DIMETHYLPIPERAZINO)-6,8-DIFLUORO-1,4-DIHYDRO-4-OXO-3-QUINOLINECARBOXYLIC ACID
  • ,5-dimethyl-1-piperazinyl)-4-oxo-,cis-
  • at4140
  • ci978
  • Clorsulon, Vetranal
  • SPARFLOXACIN, [2-14C]- 5-25 MCI(185-925 MBQ)/MMOL, DELIVERED >
  • 3-Quinolinecarboxylic acid, 5-amino-1-cyclopropyl-7-(3,5-dimethyl-1-piperazinyl)-6,8-difluoro-1,4-dihydro-4-oxo-, cis-
  • 3-Quinolinecarboxylic acid, 5-amino-1-cyclopropyl-7-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-6,8-difluoro-1,4-dihydro-4-oxo-, rel- (9CI)
  • CP 103826
  • PD 1315-1
  • Spara
  • Sparfloxacin (base and/or unspecified salts)
  • SOYISOFLAVONES
  • 5-AMINO-1-CYCLOPROPYL-7-((3S,5R)-3,5-DIMETHYLPIPERAZIN-1-YL)-6,8-DIFLUORO-4-OXO-1,4-DIHYDROQUINOLINE-3-CARBOXYLIC ACID
  • CI-978, AT-4140
  • 3-Quinolinecarboxylic acid, 5-amino-1-cyclopropyl-7-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-6,8-difluoro-1,4-dihydro-4-oxo-, rel-
  • 5-Amino-1-cyclopropyl-7-(cis-3,5-dimethyl-1-piperazinyl)-6,8-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic Acid
  • Parox
  • Zagam
  • Department of mpa of sand
  • Sparfloxacin,CI978,Inhibitor,inhibit,Antibiotic,AT 4140,Bacterial,AT4140,CI 978
  • Esparfloxacino
  • Lysine Impurity 14-d9
  • Sparfloxacin in Methanol
  • C16972650 Sparfloxacin
  • 110871-86-8
  • 3924
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