Table 7. Properties of 11 and BBR.

| Rat | Cmax or C0a (ng/mL) | AUC0-infb (ng·h/mL) | BA.c |
|---|---|---|---|
| 11 | 1085.8 ± 100.4 | 5744.7 ± 188.8 | 86.8% |
| 0.3 mg/kg p.o. | |||
| 11 | 2401.3 ± 65.6 | 6619.5 ± 2041.8 | |
| 0.3 mg/kg i.v. |
| Cebus monkeys | AUC0–24ha (μg·h/mL) | FEUAd (%) | Difference of ΔPUAefrom control (mg/dL) |
|---|---|---|---|
| 11 | 108.55 ± 52.94 | 16.5 ± 4.2 | 0.97 |
| 5 mg/kg p.o. | |||
| BBR | 95.24 ± 28.12 | 11.5 ± 7.9 | 0.46 |
| 30 mg/kg p.o. |
| In vitro evaluation | URAT1 inhibition IC50 (nM) |
|---|---|
| 11 | 37.2 |
| BBR | 190 |
Maximum concentration (Cmax or C0).
Area under the blood concentration–time curve (AUC); inf: infinity.
BA.:Bioavailability.
FEUA: Fractional excretion of urate at 0–4 h; FEUA value of control: 8.9 ± 4.0%.
ΔPUA: Changes in plasma urate level at 0–8 h; value of control: 1.65 ± 0.78 mg/dL.