An anti-TB agent; activated intracellularly via Ddn metabolism; kills M. tuberculosis by releasing RNS; active against replicating and non-replicating M. tuberculosis; inhibits growth of susceptible and mono- and multi-drug resistant M. tuberculosis clinical isolates (MICs = 0.015-5 μg/ml); decreases luminescence in the lung to in a mouse model of systemic infection with a reporter strain of M. tuberculosis at 100 mg/kg; decreases M. tuberculosis burden in the lung and spleen in an aerosol challenged guinea pig model of TB at 40 mg/kg per day

PA-824 – 5 mg

Brand:
Cayman
CAS:
187235-37-6
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

An anti-TB agent; activated intracellularly via Ddn metabolism; kills M. tuberculosis by releasing RNS; active against replicating and non-replicating M. tuberculosis; inhibits growth of susceptible and mono- and multi-drug resistant M. tuberculosis clinical isolates (MICs = 0.015-5 μg/ml); decreases luminescence in the lung to in a mouse model of systemic infection with a reporter strain of M. tuberculosis at 100 mg/kg; decreases M. tuberculosis burden in the lung and spleen in an aerosol challenged guinea pig model of TB at 40 mg/kg per day

Formal name: (6S)-6,7-dihydro-2-nitro-6-[[4-(trifluoromethoxy)phenyl]methoxy]-5H-imidazo[2,1-b][1,3]oxazine

Synonyms:  (S)-PA-824

Molecular weight: 359.3

CAS: 187235-37-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Antibiotics||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Bacterial Diseases|Tuberculosis

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