[CAS NO. 1353734-12-9] TBI-166
PRODUCTS SPECIFICATIONS [1353734-12-9]
DESCRIPTION [1353734-12-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 589.61 |
| Molecular Formula | C32H30F3N5O3 |
| SMILES | FC(F)(F)OC1=CC=C(N2C3=C/C(C(NC4=CC=CN=C4OC)=CC3=NC5=C2C=CC=C5)=N/C6CCC(OC)CC6)C=C1 |
Summary
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 9.09 mg/mL ( 15.42 mM ; ultrasonic and adjust pH to 3 with HCl)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6960 mL | 8.4802 mL | 16.9604 mL |
| 5 mM | 0.3392 mL | 1.6960 mL | 3.3921 mL |
| 10 mM | 0.1696 mL | 0.8480 mL | 1.6960 mL |
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.
