PA-824

Catalog No.S1162

PA-824 Chemical Structure

Molecular Weight(MW): 359.26

PA-824 is an anti-tuberculosis drug for tuberculosis with MIC less than 2.8 μM.Phase 2.

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Biological Activity

Description PA-824 is an anti-tuberculosis drug for tuberculosis with MIC less than 2.8 μM.Phase 2.
Features An experimental anti-tuberculosis drug.
Targets
tuberculosis [1]
In vitro

In vitro, PA-824 exhibits the high activity against multidrug-resistant clinical isolates from Asia (India and South Korea) and from throughout the United States (MIC < 1 μg/ml) and is equally active against the drug-sensitive and multidrug-resistant isolates of M. tuberculosis (MICs range, 0.039 to 0.531 μg/ml). [1] A recent study shows that single-nucleotide polymorphisms of PA-824 resistance genes (fgd1 [Rv0407] and ddn [Rv3547]) don't significantly affect the PA-824 MICs (≤ 0.25 μg/ml). [2]

In vivo In the rapid tuberculosis mouse model, PA-824 shows significant anti-microbial activity in a dose-dependent manner: at 50 mg/kg, PA-824 in MC produces a more than 1-log reduction of the CFU in the lungs; at 100 mg/kg it produces about a 2-log reduction, and at 300 mg/kg it produces a 3-log reduction. Furthermore, long-term treatment of PA-824 at 100 mg/kg in cyclodextrin/lecithin also leads to the reduction of the bacterial load below 500 CFU in the lungs and spleen. [1] PA-824 exhibits time-dependent anti-microbial activity in a murine model of tuberculosis with a maximal observed bactericidal effect of 0.1 log CFU/day over 24 days. [3]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: M. tuberculosis H37Rv
  • Concentrations: 2.0 μg/mL - 8.0 pg/mL
  • Incubation Time: 21 days
  • Method: A method is used to determine the MICs by a microdilution plate assay by using M. tuberculosis H37Rv. INH is dissolved in sterile, double-distilled water at a stock concentration of 500 μg/ml. PA-824 is dissolved in 100% dimethyl sulfoxide (DMSO) to a stock concentration of 100 μg/ml. A 1:2 dilution series of both compounds is made in a separate 96-well microtiter plate by using the same diluents. The interior 60 wells of a 96-well round-bottom microtiter assay plate are seeded with 98 μl of bacterial suspension. Two microliters of each drug is transferred to the assay plate wells containing bacteria. The final concentrations of INH in the wells range from 10.0 to 0.039 μg/mL; the final concentrations of PA-824 range from 2.0 μg/mL to 8.0 pg/mL. The assay plates are incubated at 37 °C for at least 21 days and are observed every 3 to 4 days to evaluate changes in growth. Inhibition of growth is determined both by visual examination and with a spectrophotometer at an OD600.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Gamma interferon gene-disrupted (GKO) mice are infected via a low-dose aerosol exposure to M. tuberculosis Erdman.
  • Formulation: PA-824 is formulated either in 0.5% methylcellulose (MC) or in cyclodextrin/lecithin (CM2).
  • Dosages: ≤300 mg/kg
  • Administration: Administered via p. o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 72 mg/mL (200.41 mM)
Ethanol 16 mg/mL (44.53 mM)
Water Insoluble
In vivo Add solvents individually and in order:
0.5% methylcellulose
30 mg/mL

* 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 359.26
Formula

C14H12F3N3O5

CAS No. 187235-37-6
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02422524 Suspended Tuberculosis National Institute of Allergy and Infectious Diseases (NIAID) September 2015 Phase 1
NCT02256696 Suspended Pulmonary Tuberculosis Johns Hopkins University April 2015 Phase 2
NCT02333799 Recruiting Pulmonary Tuberculosis Global Alliance for TB Drug Development March 2015 Phase 3
NCT02342886 Active, not recruiting Tuberculosis, Pulmonary, Drug Sensitive|Tuberculosis, Pulmonary, Multi Drug-resistant Global Alliance for TB Drug Development February 2015 Phase 3
NCT02193776 Active, not recruiting Tuberculosis Global Alliance for TB Drug Development November 2014 Phase 2
NCT01691534 Completed Pulmonary Tuberculosis Global Alliance for TB Drug Development October 2012 Phase 2

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID