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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|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.|
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).  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). 
|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.  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. |
|In vitro||DMSO||72 mg/mL (200.41 mM)|
|Ethanol||16 mg/mL (44.53 mM)|
|In vivo||0.5% methylcellulose||30 mg/mL|
* 1 mg/ml means slightly soluble or 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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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.
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|
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.
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