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Rifalazil

Catalog No. T16749   CAS 129791-92-0
Synonyms: KRM-1648, ABI-1648

Rifalazil is a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase. Rifalazil is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis (MIC: 0.00025 to 0.0025 μg/ml).

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Rifalazil Chemical Structure
Rifalazil, CAS 129791-92-0
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Rifalazil is a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase. Rifalazil is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis (MIC: 0.00025 to 0.0025 μg/ml).
In vitro 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[3]. Rifalazil exhibits antimicrobal activity against Gram-negative enteric bacteria, inhibits Escherichia coli and Klebsiella pneumoniae with MIC50 value of 16 and 16 μg/ml, respectively[3]. Rifalazil exhibits antimicrobal activity against non-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[3]. Rifalazil exhibits antimicrobal activity against Helicobacter pylori, Chlamydia pneumoniae and Chlamydia trachomatis with MIC50 value of 0.004, 0.000125 and 0.00025 μg/ml, respectively[3].
In vivo Rifalazil (p.o.; 20, 25, and 150 mg/kg; 6-8 weeks) combines with isoniazid 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 [2].
Synonyms KRM-1648, ABI-1648
Molecular Weight 941.07
Formula C51H64N4O13
CAS No. 129791-92-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Suchland RJ, et al. Rifalazil pretreatment of mammalian cell cultures prevents subsequent Chlamydia infection.Antimicrob Agents Chemother. 2006 Feb;50(2):439-44. 2. Shoen CM, et al. Evaluation of rifalazil in long-term treatment regimens for tuberculosis in mice.Antimicrob Agents Chemother. 2000 Jun;44(6):1458-62. 3. Rothstein DM, et al. Development potential of rifalazil.Expert Opin Investig Drugs. 2003 Feb;12(2):255-71.

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Keywords

Rifalazil 129791-92-0 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis ABI 1648 KRM-1648 ABI-1648 KRM1648 KRM 1648 ABI1648 inhibitor inhibit

 

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