产品
编 号:F563774
分子式:C10H14BCl2NO4
分子量:293.94
产品类型
结构图
CAS No: 2131798-13-3
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产品详情
生物活性:
Ganfeborole hydrochloride (GSK656) is a potent antitubercular agent, acting as an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM.
体内研究:
Ganfeborole hydrochloride shows potent antitubercular activity in mice infected with M. tuberculosis H37Rv, with ED99 of 0.4 mg/kg.
体外研究:
Ganfeborole hydrochloride is highly selective inhibitor for Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM, and shows IC50s of >300 μM and 132 μM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. Ganfeborole hydrochloride exhibits antitubercular activity with minimal inhibitory concentration (MIC) of 80 nM against Mtb H37Rv. Ganfeborole hydrochloride also exhibits EC50s of 381 μM against HepG2 cell, and 137 μM against HepG2 protein synthesis.