TBI-166, a riminophenazine analogue, is an orally active anti-tuberculosis agent with fewer adverse reactions than the lead riminophenazine compound, Clofazimine (HY-B1046) .
性状
Solid
体外研究(In Vitro)
TBI-166 抑制 M. tuberculosis H37Rv 复制 (MIC: 0.063 μg/mL),对 16 种药物敏感的临床分离株 (分枝杆菌属) 也有效,MIC 为 0.005-0.15μg/mL。 TBI-166 (0-1 μg/mL,3 天) 抑制 M. tuberculosis 感染的 J774A.1 细胞内 M. tuberculosis . has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
TBI-166 (10-80 mg/kg,口服,8 周) 在慢性小鼠 M. tuberculosis H37Rv 感染模型中表现出抗结核活性。
TBI-166 在小鼠体内显示出 LD50 值超过 3,000 mg/kg。
TBI-166 的半衰期较短 (41.25 h),可降低皮肤色素沉着的可能性。 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Xu J, et al. In Vitro and In Vivo Activities of the Riminophenazine TBI-166 against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2019 Apr 25;63(5):e02155-18. [2]. Zhu H, et al. Activity of Clofazimine and TBI-166 against Mycobacterium tuberculosis in Different Administration Intervals in Mouse Tuberculosis Models. Antimicrob Agents Chemother. 2021 Mar 18;65(4):e02164-20.
溶解度数据
In Vitro: DMSO : 9.09 mg/mL (15.42 mM; ultrasonic and adjust pH to 3 with HCl)配制储备液