Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: (6S)-6,7-dihydro-2-nitro-6-[[4-(trifluoromethoxy)phenyl]methoxy]-5H-imidazo[2,1-b][1,3]oxazine
Purity: ≥98%
Formula Markup: C14H12F3N3O5
Formula Weight: 359.3
CAS Number: 187235-37-6
Notes: PA-824 is an anti-tuberculosis (anti-TB) agent that is activated intracellularly via deazaflavin-dependent nitroreductase (Ddn) metabolism into a desnitro metabolite that kills M. tuberculosis by releasing reactive nitrogen species (RNS), including nitric oxide.{16570} It is active against replicating and non-replicating M. tuberculosis but exhibits little or no activity against M. avium, M. smegmatis, M. chelonae, and M. fortuitum.{37419} In vitro, it inhibits growth of susceptible and mono- and multi-drug resistant M. tuberculosis clinical isolates (MICs = 0.015-5 μg/ml).{37419,37420} In vivo, PA-824 (100 mg/kg per day) decreases luminescence in the lung to background levels after 60 days of treatment in a mouse model of systemic infection with a reporter strain of M. tuberculosis.{37419} It also decreases M. tuberculosis burden in the lung and spleen in an aerosol challenged guinea pig model of TB when administered at a dose of 40 mg/kg per day for 30 days.
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