Rifapentine

For research use only.

Catalog No.S1760 Synonyms: MDL473

2 publications

Rifapentine  Chemical Structure

CAS No. 61379-65-5

Rifapentine (MDL473) is an antibiotic, which inhibits DNA-dependent RNA polymerase activity, used to treat tuberculosis.

Selleck's Rifapentine has been cited by 2 publications

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Biological Activity

Description Rifapentine (MDL473) is an antibiotic, which inhibits DNA-dependent RNA polymerase activity, used to treat tuberculosis.
Targets
DNA-dependent RNA polymerase [1]
In vitro

Rifapentine inhibits the function of DNA-dependent RNA polymerase in strains of M. tuberculosis, while inducing no effect on mammalian cells. Both Rifapentine and its active metabolite, 25-desacetylrifapentine, localize within monocyte-derived macrophages, thus allowing for intracellular inhibition of M. tuberculosis at a greater kill rate as compared with that of the parent or metabolite alone. Rifapentine is deacetylated in the liver and induces cytochrome P450 much less than rifampin. [1] Rifapentine has shown higher bacteriostatic and bactericidal activities (MICs and MBCs) than RMP, especially against intracellular bacteria growing in human monocyte-derived macrophages. [2]

In vivo Rifapentine inhibits bacterial RNA synthesis by binding to the β-subunit of DNA-dependent RNA polymerase in susceptible species. Rifapentine is generally more active than rifampicin against sensitive strains of M. tuberculosis. [3] Rifapentine significantly increases the rate of antipyrine and pentobarbital metabolism in vivo. Rifapentine also increases liver weight, the content of liver microsomal protein and cytochrome P-450, the activity of NADPH-cytochrome C reductase and NADPH oxidase. [4] Rifapentine combined with isoniazid (INH) and pyrazinamide (PZA) administered daily results in an apparent clearance of M.tuberculosis organisms in the lungs and spleens of infected mice after 10 weeks of treatment. [5]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (114.02 mM)
Ethanol 17 mg/mL (19.38 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 877.03
Formula

C47H64N4O12

CAS No. 61379-65-5
Storage powder
in solvent
Synonyms MDL473
Smiles CC1C=CC=C(C(=O)NC2=C(C(=C3C(=C2O)C(=C(C4=C3C(=O)C(O4)(OC=CC(C(C(C(C(C(C1O)C)O)C)OC(=O)C)C)OC)C)C)O)O)C=NN5CCN(CC5)C6CCCC6)C

In vivo Formulation Calculator (Clear solution)

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03730181 Active not recruiting Drug: Rifapentine|Drug: Isoniazid Latent Tuberculosis Centers for Disease Control and Prevention|University of Stellenbosch|Johns Hopkins University|Sanofi|University of Cape Town|Chris Hani Baragwanath Academic Hospital|Washington D.C. Veterans Affairs Medical Center October 12 2019 Phase 1|Phase 2
NCT04094012 Recruiting Drug: isoniazid and rifapentine Latent Tuberculosis Infection National Taiwan University Hospital September 24 2019 Phase 3
NCT01690403 Completed Drug: rifapentine (M000473)|Drug: EFZ EMT TDF Tuberculosis Sanofi December 2012 Phase 1
NCT01574638 Completed Drug: Rifapentine (RPT) Tuberculosis National Institute of Allergy and Infectious Diseases (NIAID) June 2012 Phase 1
NCT00814671 Completed Drug: Rifapentine 450|Drug: Rifapentine 600|Drug: Rifampin Tuberculosis Johns Hopkins University|University of Cape Town Lung Institute|University of Cape Town April 2010 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID