Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Rifapentine

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Rifapentine DNA/RNA Synthesis inhibitor

Cat.No.S1760

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

Chemical Structure

Molecular Weight: 877.03

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Quality Control

Batch: Purity: >97%
97

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (114.02 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

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In vivo
Batch:

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.

Chemical Information, Storage & Stability

Molecular Weight 877.03 Formula

C47H64N4O12

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

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

Mechanism of Action

Targets/IC50/Ki
DNA-dependent RNA polymerase
In vitro
Rifapentine inhibits the function of DNA-dependent RNA polymerase in strains of M. tuberculosis, while inducing no effect on mammalian cells. Both this compound 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. It is deacetylated in the liver and induces cytochrome P450 much less than rifampin. This chemical has shown higher bacteriostatic and bactericidal activities (MICs and MBCs) than RMP, especially against intracellular bacteria growing in human monocyte-derived macrophages.
In vivo
Rifapentine inhibits bacterial RNA synthesis by binding to the β-subunit of DNA-dependent RNA polymerase in susceptible species. This compound is generally more active than rifampicin against sensitive strains of M. tuberculosis. It significantly increases the rate of antipyrine and pentobarbital metabolism in vivo. This chemical also increases liver weight, the content of liver microsomal protein and cytochrome P-450, the activity of NADPH-cytochrome C reductase and NADPH oxidase. When combined with isoniazid (INH) and pyrazinamide (PZA) administered daily, it results in an apparent clearance of M.tuberculosis organisms in the lungs and spleens of infected mice after 10 weeks of treatment.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/2319833/
  • [5] https://pubmed.ncbi.nlm.nih.gov/10508006/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06281834 Not yet recruiting
Pediatric HIV Infection|Latent Tuberculosis
Brigham and Women''s Hospital|APIN Public Health Initiatives|University of Cape Town
 May 2024 Phase 1
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

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