Molecular Formula | C17H16F3N3O5S |
Molar Mass | 431.39 |
Density | 1.68 |
Melting Point | 190-191°C |
Solubility | DMSO: 13.3 mg/mL |
Appearance | Solid |
Color | White to Pale Yellow |
Storage Condition | -20°C Freezer |
In vitro study | The MIC of BTZ043 against M. tuberculosis H37Rv and Mycobacterium smegmatis are 1 ng/mL (2.3 nM) and 4 ng/mL (9.2 nM), respectively. The in vitro activity of BTZ043 against 30 Nocardia brasiliensis isolates is also tested. The MIC50 and MIC90 values for BTZ043 are 0.125 and 0.25 μg/mL. The MIC for N. carnea ATCC 6847 is 0.003μg/mL, for N. transvalensis ATCC 6865 is 0.003μg/mL, for N. brasiliensis NCTC10300 is 0.03 μg/mL, and for N. brasiliensis HUJEG-1 is 0.125μg/mL. The MIC value for M. tuberculosis H37Rv is 0.000976 μg/mL. The MIC value of BTZ-043 is >64 μg/mL for Escherichia coli ATCC 25922 and S. aureus ATCC 29213. |
In vivo study | Four weeks of treatment with BTZ043 reduces the bacterial burden in the lungs and spleens by 1 and 2 logs, respectively, at the concentrations used. Additional results suggest that BTZ043 efficacy is time-rather than dose-dependent. Acute (5 g/kg) and chronic (25 and 250 mg/kg) toxicology studies in uninfected mice show that, even at the highest dose tested, there are no adverse anatomical, behavioral, or physiological effects after one month. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.318 ml | 11.591 ml | 23.181 ml |
5 mM | 0.464 ml | 2.318 ml | 4.636 ml |
10 mM | 0.232 ml | 1.159 ml | 2.318 ml |
5 mM | 0.046 ml | 0.232 ml | 0.464 ml |