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TBI-166

Names

[ CAS No. ]:
1353734-12-9

[ Name ]:
TBI-166

Biological Activity

[Description]:

TBI-166, a riminophenazine analogue, is an orally active anti-tuberculosis agent with fewer adverse reactions than the lead riminophenazine compound, Clofazimine (HY-B1046) [1][2][3].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Bacterial

[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[1]。 TBI-166 (0-1 μg/mL，3 天) 抑制 M. tuberculosis 感染的 J774A.1 细胞内 M. tuberculosis[1].

[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[1]。 TBI-166 在小鼠体内显示出 LD50 值超过 3,000 mg/kg[1]。 TBI-166 的半衰期较短 (41.25 h)，可降低皮肤色素沉着的可能性[2]。 Animal Model: Chronic murine M. tuberculosis H37Rv infected model[1] Dosage: 10, 20, 80 mg/kg Administration: Oral administration, 8 weeks. Result: Reduced CFU counts in lung.

[References]

[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.  

[3]. Ding Y, et al. Superior Efficacy of a TBI-166, Bedaquiline, and Pyrazinamide Combination Regimen in a Murine Model of Tuberculosis. Antimicrob Agents Chemother. 2022 Sep 20;66(9):e0065822.  

Chemical & Physical Properties

[ Molecular Formula ]:
C32H30F3N5O3

[ Molecular Weight ]:
589.61

Related Compounds