For research use only.
CAS No. 187235-37-6
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||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02333799||Completed||Drug: Bedaquiline|Drug: PA-824|Drug: Linezolid||Pulmonary Tuberculosis||Global Alliance for TB Drug Development||March 2015||Phase 3|
|NCT01674218||Completed||Drug: Moxifloxacin|Drug: PA-824|Other: Placebo||Tuberculosis||National Institute of Allergy and Infectious Diseases (NIAID)||September 2012||Phase 1|
|NCT01768273||Completed||Drug: Midazolam|Drug: PA-824||Tuberculosis||Global Alliance for TB Drug Development||December 2009||Phase 1|
|NCT03202693||Completed||Drug: PA-824||Tuberculosis||Global Alliance for TB Drug Development||March 2006||Phase 1|
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