187235-37-6
(S)-PA 824
CAS: 187235-37-6
Molecular Formula: C14H12F3N3O5
187235-37-6 - Names and Identifiers
187235-37-6 - Physico-chemical Properties
| Molecular Formula | C14H12F3N3O5 |
| Molar Mass | 359.26 |
| Density | 1.58 |
| Melting Point | 149-150℃ |
| Boling Point | 462.3±55.0 °C(Predicted) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | powder |
| Color | white to brown |
| pKa | -0.67±0.40(Predicted) |
| Storage Condition | -20°C |
| In vitro study | In vitro, PA-824 showed high activity against multidrug-resistant clinical strains from Asia (India and Korea) and the United States (MIC < 1 μg/ml), it was also effective against drug-sensitive and multidrug-resistant strains of M. Tuberculosis (MICs range, 0.039 to 0.531 μg/ml). A recent study showed no significant effect of single nucleotide polymorphisms in the PA-824 resistance genes (fgd1 [Rv0407] and ddn [Rv3547]) on PA-824 MICs (≤ 0.25 μg/ml). |
| In vivo study | In a mouse model of acute pulmonary tuberculosis, PA-824 showed a significant dose-dependent antitumor activity: PA-824,50 mg/kg of MC produced a more than 1-log reduction in lung CFU; 100 mg/kg, produced a 2-log reduction; 300 mg/kg, produced a 3-log reduction. In addition, long-term treatment in cyclodextrin/lecithin PA-824(100 mg/kg) resulted in reduced bacterial load below 500 CFU in lung and spleen. In a mouse model of pulmonary tuberculosis, PA-824 exhibited time-dependent antibacterial activity with a maximum bactericidal effect of 0.1 log CFU/day observed over 24 days. |
187235-37-6 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.783 ml | 13.917 ml | 27.835 ml |
| 5 mM | 0.557 ml | 2.783 ml | 5.567 ml |
| 10 mM | 0.278 ml | 1.392 ml | 2.783 ml |
| 5 mM | 0.056 ml | 0.278 ml | 0.557 ml |
Last Update：2024-01-02 23:10:35
187235-37-6 - Reference Information
| use | (S)-6, 7-dihydro-2-nitro -6-[[4-(trifluoromethoxy) phenyl] methoxy]-5H-imidazo [2,1-B][1,3] Oxazine (PA-824) is a new anti-tuberculosis drug. |
| biological activity | PA-824 is an anti-tuberculosis drug that acts on tuberculosis with a MIC of <1 μg/mL. Phase 2. |
| target | TargetValue tuberculosis |
| Target | Value |
| in vitro study | in vitro, PA-824 showed high activity against multidrug-resistant clinical strains from Asia (India and South Korea) and the United States (MIC < 1 μg/ml), and was equally effective against drug-sensitive and multidrug-resistant tuberculosis strains (MICs range, 0.039 to 0.531 μg/ml). A recent study showed that single nucleotide polymorphisms of PA-824 drug resistance genes (fgd1 [Rv0407] and ddn [Rv3547]) had no significant effect on PA-824 MICs (≤ 0.25 μg/ml). |
| in vivo study | in the mouse model of acute pulmonary tuberculosis, the PA-824 showed significant dose-dependent anti-tumor activity: the PA-824 dissolved in MC, 50 mg/kg, resulting in a decrease in CFU production in the lung over 1-log; 100 mg/kg, resulting in a decrease in 2-log production; 300 mg/kg, resulting in a decrease in 3-log. In addition, long-term treatment of PA-824(100 mg/kg) in cyclodextrin/lecithin resulted in a decrease in bacterial load, which was lower than 500 CFU in lung and spleen. In the mouse model of pulmonary tuberculosis, the PA-824 showed time-dependent antibacterial activity, and the maximum bactericidal effect observed in 24 days was 0.1 log CFU/day. |
Last Update：2024-04-10 22:30:50
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View History
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