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DprE1-IN-1 demonstrats efficacy in a rodent model of tuberculosis, making it promising for further development. The pharmacokinetic profile of DprE1-IN-1 as a representative of the series in mice, rats, and dogs was determined after i.v. and oral dosing. DprE1-IN-1 shows oral bioavailabilities of 86% and 100% in rats and dogs, respectively. The oral exposures of DprE1-IN-1, assessed in infected animals, shows AUCs ranging from 166 to 240 μM · h, and free plasma concentrations were maintained above the MIC for 10 to 24 h.
| Molecular Weight | 355.39 |
| Formula | C18H21N5O3 |
| CAS Number | 1494675-86-3 |
| Form | Solid |
| Solubility (25°C) | 11 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Shirude PS, et al. J Med Chem. Lead optimization of 1,4-azaindoles as antimycobacterial agents.
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