CAS 129791-92-0|Rifalazil

Introduction：Basic information about CAS 129791-92-0|Rifalazil, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Rifalazil BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	Rifalazil
CAS Number	129791-92-0	Molecular Weight	941.07300
Density	1.36g/cm3	Boiling Point	1048.6ºC at 760mmHg
Molecular Formula	C₅₁H₆₄N₄O₁₃	Melting Point	195-200° (dec)
MSDS	/	Flash Point	588ºC

Names

Name	Rifalazil
Synonym	More Synonyms

Rifalazil BiologicalActivity

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 pylori, C. 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].
Related Catalog	Research Areas >>InfectionSignaling Pathways >>Cell Cycle/DNA Damage >>DNA/RNA SynthesisResearch Areas >>Inflammation/ImmunologySignaling Pathways >>Anti-infection >>Bacterial
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.
References	[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.

Chemical & Physical Properties

Density	1.36g/cm3
Boiling Point	1048.6ºC at 760mmHg
Melting Point	195-200° (dec)
Molecular Formula	C₅₁H₆₄N₄O₁₃
Molecular Weight	941.07300
Flash Point	588ºC
Exact Mass	940.44700
PSA	230.66000
LogP	6.57360
Vapour Pressure	0mmHg at 25°C
Index of Refraction	1.634
InChIKey	IXSVOCGZBUJEPI-QEOGJXKSSA-N
SMILES	COC1C=COC2(C)Oc3c(C)c(O)c4c(=O)c(c5oc6cc(N7CCN(CC(C)C)CC7)cc(=O)c6nc5c4c3=C2O)NC(=O)C(C)=CC=CC(C)C(O)C(C)C(O)C(C)C(OC(C)=O)C1C

Synonyms

krm 1648

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