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. 2020 Jul 15;11(10):2017–2023. doi: 10.1021/acsmedchemlett.0c00176

Table 7. Properties of 11 and BBR.

graphic file with name ml0c00176_0010.jpg

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
a

Maximum concentration (Cmax or C0).

b

Area under the blood concentration–time curve (AUC); inf: infinity.

c

BA.:Bioavailability.

d

FEUA: Fractional excretion of urate at 0–4 h; FEUA value of control: 8.9 ± 4.0%.

e

ΔPUA: Changes in plasma urate level at 0–8 h; value of control: 1.65 ± 0.78 mg/dL.