For research use only. Not for therapeutic Use.
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].
TBI-166 inhibits M. tuberculosis H37Rv replicates (MIC: 0.063 μg/mL), and is effective against 16 drug-sensitive clinical isolates (Mycobacterial species) with MICs of 0.005-0.15 μg/mL[1].
TBI-166 (0-1 μg/mL, 3 days) inhibits intracellular M. tuberculosis in M. tuberculosis infecting J774A.1 cells[1].
TBI-166 (10-80 mg/kg, p.o., 8 weeks) displays antituberculosis activity in chronic murine M. tuberculosis H37Rv infected model[1].
TBI-166 displays a LD50 more than 3,000 mg/kg in mice[1].
TBI-166 has a short half-life (41.25 h) and reduces the potential for skin pigmentation[2].
| Catalog Number | I041772 |
| CAS Number | 1353734-12-9 |
| Synonyms | 3-(4-methoxycyclohexyl)imino-N-(2-methoxypyridin-3-yl)-5-[4-(trifluoromethoxy)phenyl]phenazin-2-amine |
| Molecular Formula | C32H30F3N5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C32H30F3N5O3/c1-41-22-13-9-20(10-14-22)37-27-19-30-28(18-26(27)39-25-7-5-17-36-31(25)42-2)38-24-6-3-4-8-29(24)40(30)21-11-15-23(16-12-21)43-32(33,34)35/h3-8,11-12,15-20,22,39H,9-10,13-14H2,1-2H3 |
| InChIKey | GUSGYHIQYWRCQO-UHFFFAOYSA-N |
| SMILES | COC1CCC(CC1)N=C2C=C3C(=NC4=CC=CC=C4N3C5=CC=C(C=C5)OC(F)(F)F)C=C2NC6=C(N=CC=C6)OC |
| Reference | [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. |
