| Identification | Back Directory | [Name]
2-Phenazinamine, 3,5-dihydro-3-[(4-methoxycyclohexyl)imino]-N-(2-methoxy-3-pyridinyl)-5-[4-(trifluoromethoxy)phenyl]- | [CAS]
1353734-12-9 | [Synonyms]
TBI-166
3-((4-Methoxycyclohexyl)imino)-N-(2-methoxypyridin-3-yl)-5-(4-(trifluoromethoxy)phenyl)-3,5-dihydrophenazin-2-amine
2-Phenazinamine, 3,5-dihydro-3-[(4-methoxycyclohexyl)imino]-N-(2-methoxy-3-pyridinyl)-5-[4-(trifluoromethoxy)phenyl]- | [Molecular Formula]
C32H30F3N5O3 | [MOL File]
1353734-12-9.mol | [Molecular Weight]
589.61 |
| Chemical Properties | Back Directory | [Boiling point ]
623.0±55.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
9.46±0.70(Predicted) | [color ]
Brown to reddish brown |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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].
| 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. DOI:10.1128/AAC.02155-18
[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. DOI:10.1128/AAC.02164-20
[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. DOI:10.1128/aac.00658-22 |
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