Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Rifapentine For research use only.

Rifapentine

Synonyms: MDL473

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

Rifapentine Chemical Structure

Rifapentine Chemical Structure

CAS: 61379-65-5

Selleck's Rifapentine has been cited by 3 publications

Purity & Quality Control

Batch: Purity: >97%
97

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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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05655702 Recruiting Tuberculosis ANRS Emerging Infectious Diseases|Haiphong University of Medicine and Pharmacy|Expertise France|Université Montpellier|New York University|CENTER FOR SUPPORTING COMMUNITY DEVELOPMENT INITIATIVES October 2 2023 Not Applicable
NCT03730181 Recruiting 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 Completed Latent Tuberculosis Infection National Taiwan University Hospital September 24 2019 Phase 3
NCT01690403 Completed Tuberculosis Sanofi December 2012 Phase 1
NCT01574638 Completed Tuberculosis National Institute of Allergy and Infectious Diseases (NIAID) June 2012 Phase 1

Chemical lnformation & Solubility

Molecular Weight 877.03 Formula

C47H64N4O12
CAS No. 61379-65-5 SDF Download Rifapentine SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (114.02 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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