中文名 | BTZ043 |
英文名 | BTZ043 |
别名 | 化合物BTZ043 DPRE1抑制剂(BTZ043) DPRE1抑制剂(PBTZ169) 2-[(2S)-2-甲基-1,4-二氧杂-8-氮杂螺[4.5]癸烷-8-基]-8-硝基-6-三氟甲基-4H-1,3-苯并噻嗪-4-酮 |
英文别名 | BTZ043 CS-2310 PBTZ 169 BTZ 10526043 BTZ043 raceMate BTZ043 (BTZ-043 2-[(3S)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one 2-[(2S)-2-Methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-trifluoromethyl-4H-1,3-benzothiazin-4-one |
CAS | 1161233-85-7 |
化学式 | C17H16F3N3O5S |
分子量 | 431.39 |
密度 | 1.68 |
熔点 | 190-191°C |
溶解度 | 氯仿 (微溶),甲醇 (非常微溶) |
存储条件 | -20°C Freezer |
外观 | 固体 |
颜色 | White to Pale Yellow |
体外研究 | 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. |
体内研究 | 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 |
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