1. Cell Cycle/DNA Damage
    Anti-infection
  2. DNA/RNA Synthesis
    Bacterial
  3. Rifalazil

Rifalazil (Synonyms: KRM-1648; ABI-1648)

Cat. No.: HY-105099
Handling Instructions

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 pyloriC. 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).

For research use only. We do not sell to patients.

Rifalazil Chemical Structure

Rifalazil Chemical Structure

CAS No. : 129791-92-0

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Description

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[1]. Rifalazil (KRM-1648; ABI-1648) is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pyloriC. pneumoniae and C. trachomatis with MIC values from 0.00025 to 0.0025 μg/ml[3]. Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of Chlamydia infection, Clostridium difficile associated diarrhea (CDAD), and tuberculosis (TB)[2].

IC50 & Target

IC50: RNA polymerase[1]

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 (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[2].

Animal Model: Female CD-1 mice infected with 5.2 × 107 viable mycobacteria[2]
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.
Clinical Trial
Molecular Weight

941.07

Formula

C₅₁H₆₄N₄O₁₃

CAS No.

129791-92-0

SMILES

CC(C)CN(CC1)CCN1C2=CC(O3)=C(C(O)=C2)N=C(C3=C(NC(/C(C)=C\C=C\[[email protected]@H]([[email protected]](O)[[email protected]@H](C)[[email protected]@H](O)[[email protected]@H](C)[[email protected]@H]([[email protected]@H]([[email protected]](/C=C/O[[email protected]@]4(C)O5)OC)C)OC(C)=O)C)=O)C6=O)C7=C6C(O)=C(C)C5=C7C4=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

RifalazilKRM-1648ABI-1648KRM1648KRM 1648ABI1648ABI 1648DNA/RNA SynthesisBacterialAntibioticChlamydia,?infectionClostridiumdifficileassociateddiarrheaCDADtuberculosisbacterialInhibitorinhibitorinhibit

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