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BTZ043

CAS No. : 1161233-85⁻⁷

MCE 国际站：BTZ043

产品活性：BTZ043 是 DprE1 的抑制剂，它对结核分枝杆菌 H37Rv (M. tuberculosis H37Rv) 和耻垢分枝杆菌 (Mycobacterium smegmatis) 的 MIC 值分别为 2.3 nM 和 9.2 nM。

研究领域：Anti-infection

作用靶点：Bacterial | Antibiotic

In Vitro: 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: 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.

相关产品：Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Anti-Infection Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Antibacterial Compound Library | Antibiotics Library | Rapamycin | Doxorubicin hydrochloride | Bafilomycin A1 | Puromycin dihydrochloride | Cycloheximide | Chloroquine | Staurosporine | Dexamethasone | Doxycycline (hyclate) | Actinomycin D | Cyclosporin A | G-418 disulfate | 5-Azacytidine | Etoposide | Mitomycin C | CCCP | Nigericin sodium salt | Brefeldin A | Wortmannin | Resveratrol | Tunicamycin | Bleomycin sulfate | Hygromycin B | Tacrolimus | Ionomycin | Vancomycin hydrochloride | Streptozocin | Tanespimycin | Oligomycin A

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