产品
编 号：F112509
分子式：C51H64N4O13
分子量：941.07
分子式：C51H64N4O13
分子量：941.07
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 129791-92-0
产品详情
生物活性：
Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in?RNA polymerase. Rifalazil (KRM-1648; ABI-1648) is an?antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria,?Helicobacter pylori,?C. pneumoniae?and?C. trachomatis?with MIC values from 0.00025 to 0.0025 μg/ml. Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of?Chlamydia?infection,?Clostridium difficile?associated diarrhea?(CDAD), and?tuberculosis?(TB).
体内研究：
Rifalazil (oral gavage; 20, 25, and 150 mg/kg; 6-8 weeks) combines with isoniazid (INH) for 6 weeks or greater significantly reduced the number of mice per group in which?M. tuberculosis?is detected in both spleens and lungs compared to the reductions for the early and late controls. And the addition of Pyrazinamide (PZA) does not significantly improve RLZ-INH therapy at any time point.Animal Model:Female CD-1 mice infected with 5.2 × 107?viable mycobacteria
Dosage:20, 25, and 150 mg/kg; 6-8 weeks
Administration:Oral gavage
Result:Combined with isoniazid (INH) showed its potential for short-course treatment of?Mycobacterium tuberculosis?infection.
体外研究：
Rifalazil exhibits antimicrobal activity against Gram-positive enteric bacteria, inhibits Clostridium difficile, Clostridium perfringens, Bacteroides fragilis with MIC50 value of 0.0015, 0.0039, 0.0313 μg/ml, respectively.Rifalazilexhibits antimicrobal activity against Gram-negative enteric bacteria, inhibits Escherichia coli and Klebsiella pneumoniae with MIC50 value of16 and 16 μg/ml, respectively.Rifalazilexhibits antimicrobal activity againstnon-enteric Gram-positive bacteria, inhibits Methicillin-susceptible Staphylococcus aureus, Methicillin-resistant S. aureus, Methicillin- and quinolone-resistant S. aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae with MIC50 value of 0.0078, 0.0078, 0.0078, 0.0078, 0.0002, 0.0001 μg/ml, respectively.Rifalazilexhibits antimicrobal activity against Helicobacter pylori, Chlamydia pneumoniae and Chlamydia trachomatis with MIC50 value of0.004, 0.000125 and 0.00025 μg/ml, respectively.
Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in?RNA polymerase. Rifalazil (KRM-1648; ABI-1648) is an?antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria,?Helicobacter pylori,?C. pneumoniae?and?C. trachomatis?with MIC values from 0.00025 to 0.0025 μg/ml. Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of?Chlamydia?infection,?Clostridium difficile?associated diarrhea?(CDAD), and?tuberculosis?(TB).
体内研究：
Rifalazil (oral gavage; 20, 25, and 150 mg/kg; 6-8 weeks) combines with isoniazid (INH) for 6 weeks or greater significantly reduced the number of mice per group in which?M. tuberculosis?is detected in both spleens and lungs compared to the reductions for the early and late controls. And the addition of Pyrazinamide (PZA) does not significantly improve RLZ-INH therapy at any time point.Animal Model:Female CD-1 mice infected with 5.2 × 107?viable mycobacteria
Dosage:20, 25, and 150 mg/kg; 6-8 weeks
Administration:Oral gavage
Result:Combined with isoniazid (INH) showed its potential for short-course treatment of?Mycobacterium tuberculosis?infection.
体外研究：
Rifalazil exhibits antimicrobal activity against Gram-positive enteric bacteria, inhibits Clostridium difficile, Clostridium perfringens, Bacteroides fragilis with MIC50 value of 0.0015, 0.0039, 0.0313 μg/ml, respectively.Rifalazilexhibits antimicrobal activity against Gram-negative enteric bacteria, inhibits Escherichia coli and Klebsiella pneumoniae with MIC50 value of16 and 16 μg/ml, respectively.Rifalazilexhibits antimicrobal activity againstnon-enteric Gram-positive bacteria, inhibits Methicillin-susceptible Staphylococcus aureus, Methicillin-resistant S. aureus, Methicillin- and quinolone-resistant S. aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae with MIC50 value of 0.0078, 0.0078, 0.0078, 0.0078, 0.0002, 0.0001 μg/ml, respectively.Rifalazilexhibits antimicrobal activity against Helicobacter pylori, Chlamydia pneumoniae and Chlamydia trachomatis with MIC50 value of0.004, 0.000125 and 0.00025 μg/ml, respectively.
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