| Name | OPC-167832 |
| Description | OPC-167832 is a highly potent and orally bioavailable dprE1 inhibitor with an IC₅₀ of 0.258 μM. It exhibits anti-mycobacterial activity against Mycobacterium tuberculosis and can be used in tuberculosis-related research. |
| In vitro | Methods: In vitro drug sensitivity testing of OPC-167832 was performed on Mycobacterium tuberculosis and various standard strains, and its bacteriostatic and bactericidal activities against intracellular Mycobacterium tuberculosis were determined.
Results：
1 OPC-167832 exhibited potent inhibitory activity against the Mycobacterium tuberculosis laboratory strains H37Rv and Kurono, with a MIC of 0.0005 μg/mL for both, while it had almost no antibacterial activity against standard strains of aerobic and anaerobic non-mycobacterial bacteria.
2 The IC₉₀ of OPC-167832 against intracellular Mycobacterium tuberculosis was less than 100%, and the bacteriostatic concentrations against H37Rv and Kurono strains were 0.0048 μg/mL and 0.0027 μg/mL, respectively; it could exert intracellular bactericidal effect at low concentrations, and the bactericidal activity tended to be saturated when the concentration was ≥0.004 μg/mL [1]. |
| In vivo | Methods: OPC-167832 was administered orally at doses of 0.625–10 mg/kg to detect its pharmacokinetics and lung tissue distribution; oral administration at the same doses was performed for 4 weeks to observe changes in lung tissue CFU; intragastric administration of 2.5 mg/kg combined with DCMB was conducted for 12 weeks to evaluate the combined therapeutic effect.
Results：
1 OPC-167832 had good pharmacokinetic properties after oral administration, with a time to peak concentration (tmax) of 0.5–1.0 h and an elimination half-life (t1/2) of 1.3–2.1 h; the drug concentration in the lungs was approximately twice that in the plasma, and the Cmax and AUCt in both plasma and lungs were dose-dependent.
2 Compared with the vehicle group, OPC-167832 (0.625–10 mg/kg, oral administration, 4 weeks) significantly reduced lung CFU, and the lung CFU decreased in a dose-dependent manner within the dose range of 0.625–2.5 mg/kg.
3 OPC-167832 (2.5 mg/kg, intragastric administration, combined with DCMB, 12 weeks) showed the optimal therapeutic effect; the lung CFU of mice was below the detection limit after 6 weeks of treatment, and the lung bacteria of all mice were eradicated after 8 weeks of treatment [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 144 mg/mL (315.21 mM), Sonication is recommended.
|
| Keywords | OPC-167832 |
| Inhibitors Related | Neomycin sulfate | Adipic dihydrazide | Levulinic acid | D(+)-Raffinose pentahydrate | Sulfamethoxazole sodium | Terbinafine hydrochloride | Doxycycline | Hyaluronic acid sodium (MW 20 kDa) | Dimethyl sulfoxide | Sodium diacetate | Sodium bicarbonate | BES |
United States
