Detail of "127254-12-0"

CAS Number:
127254-12-0
Name:
3-Quinolinecarboxylicacid,7-[(7S)-7-amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-1,4-dihydro-4-oxo-
Superlist Name:
Sitafloxacin
Molecular Structure:
Formula:
C₁₉H₁₈ClF₂N₃O₃
Molecular Weight:
409.81
Synonyms:
3-Quinolinecarboxylicacid,7-(7-amino-5-azaspiro[2.4]hept-5-yl)-8-chloro-6-fluoro-1-(2-fluorocyclopropyl)-1,4-dihydro-4-oxo-,[1R-[1a(S*),2a]]-;DU 6859;DU 6859a;Gracevit;
Density:
1.63 g/cm³
Boiling Point:
629.2 °C at 760 mmHg
Flash Point:
334.3 °C

Famous Chemical Enterprises

Livzon
Total
Shell
Dupont
Exxonmobil
Akzonobel
Basf
Bayer
BP

Other Products

Supplier Location
Supplier Location
- China (Mainland)(21)
- United States(1)
Business Type
Business Type
- Lab/Research institutions(5)
- Manufacturers(1)
- Trading Company(16)
Certificates
Certificates
- ISO(2)
- Production License(1)

Please post your buying leads>>

Display：

Manufacturer
Enterprise Authentication
Suppiers of more reward points first
New supplier

Please post your buying leads,so that our qualified suppliers will soon contact you!
*Required Fields

Reference

Pharmacokinetics, tissue distribution, and excretion of sitafloxacin, a new fluoroquinolone antibiotic, in rats, dogs, and monkeys: Pharmacokinetics, tissue distribution, and excretion of sitafloxacin, a new fluoroquinolone antibiotic, in rats, dogs, and monkeys. Tachibana, Masaya; Tanaka, Makoto; Mitsugi, Koichi; Jin, Yoshitaka; Takaichi, Matsuo; Okazaki, Osamu (Drug Metabolism and Physicochemical Property Research Laboratories, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan). Arzneimittel Forschung, 54(12), 898-905 (English) 2004 Editio Cantor Verlag. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The pharmacokinetics, tissue distribution and excretion of sitafloxacin (CAS 127254-12-0, DU-6859a) were investigated in rats, dogs, and monkeys following single i.v. or single oral administration of 14C-labeled sitafloxacin at a dose of 4.69 mg/kg. Following single administration of the oral dose, serum concns. of radioactivity peaked at 0.5 h in rats, 2.3 h in dogs, and 2.5 h in monkeys. The apparent absorption ratios of 14C-sitafloxacin based on the AUC0-￥ were 31 %, 51 %, and 93 % in rats, dogs, and monkeys, resp. In rats, the drug-related radioactivity had been distributed to most organs and tissues 30 min after oral dosing, and had been essentially eliminated after 24 h. The highest levels of radioactivity were obsd. in the kidneys and liver, whereas the concns. in the cerebrum and spinal cord were much lower than the serum value. The urinary recoveries of radioactivity after i.v. dosing were 45.5 % in rats, 32.3 % in dogs, and 77.8 % in monkeys. In bile duct-cannulated rats, 57.8 % of the orally administered radioactivity was excreted in the bile within 48 h, and at least 45 % of the sitafloxacin-related material secreted in the bile was re-absorbed from the gastrointestinal tract. These results indicate that sitafloxacin is rapidly absorbed and widely distributed into various tissues. Sitafloxacin-related material is eliminated primarily through both renal and biliary excretion in rats, and possibly in dogs, whereas renal excretion is the major route of elimination in monkeys.

Experimental estimation of breakpoint MIC of antimicrobial chemotherapy: Experimental estimation of breakpoint MIC of antimicrobial chemotherapy. Study on breakpoint MIC of DU-6859a (50 mg twice daily) for moderately complicated urinary tract infection. Nishimura, Masahiro; Takahashi, Satoshi; Sano, Masato; Hirose, Takaoki; Tsukamoto, Taiji; Kumamoto, Yoshiaki (Saka Urol. Hosp., Sapporo 001, Japan). Nippon Kagaku Ryoho Gakkai Zasshi, 45(1), 1-8 (Japanese) 1997 Nippon Kagaku Ryoho Gakkai. CODEN: NKRZE5. ISSN: 1340-7007. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 10 We exptl. investigated an effective method of antimicrobial chemotherapy utilizing a new form of oral fluoroquinoline, DU-6859a, for the treatment of moderately cases of complicated urinary tract infection (UTI) without an indwelling a catheter. Prior to the clin. investigation, an in vitro investigation was performed using an exptl. 127254-12-0 and 13721-01-2 are cas registry numbers. These chemicals are also mentioned in this article. model of moderately complicated UTI. This computer-controlled model can simulate fluctuations in the urinary concn. of antimicrobials. As a result of the in vitro investigation, we decided upon a regimen of DU-6859a. Afterwards, a clin. investigation utilizing this regimen was performed, and the results were then compared. We examd. the MIC70 of DU-6859a with bacteria isolated from non-catheterized complicated UTI patients. The MIC70 was 0.5 mg/mL. According to our previous reports, this regimen, in which the breakpoint MIC is higher than the MIC70 of causative bacteria, is effective for clin. treatment. The breakpoint MIC of the regimen, 50 mg DU-6859a twice per day, was measured using our exptl. model. Pseudomonas aeruginosa strains, whose MICs were lower than 2 mg/mL, and Enterococcus faecalis strains, whose MICs were lower than 2 mg/mL, were eradicated utilizing this regimen. Thus, the breakpoint MIC of this regimen was 2 mg/mL, having a higher value than the MIC70 described above. These results suggest that this regimen is effective for clin. treatment. A clin. investigation was also performed utilizing a regimen of 50 mg DU-6859a twice per day. The eradication rate was 85.4% (41/48), and the efficacy rate was 85.4% (41/48). These results suggest that this regimen of DU-6859a, as detd. by our exptl. model, is effective for clin. treatment. Utilizing our exptl. model makes it possible to det. the most effective regimen for the treatment of moderately complicated UTI prior to clin. treatment. .

Detail of "127254-12-0"

3-Quinolinecarboxylicacid,7-[(7S)-7-amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-1,4-dihydro-4-oxo-

Famous Chemical Enterprises

Related products

Other Products

Supplier Location

Business Type

Certificates

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

CAS No.127254-12-0 Sitafloxacin

Reference