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. 2018 Aug 27;62(9):e00012-18. doi: 10.1128/AAC.00012-18

TABLE 2.

In vitro metabolism, protein binding, blood/plasma ratio, and plasma stability data for UCT943a

Parameter Value for the parameter (SD) in:
Human Dog Rat Mouse
Microsomal CLint (μl/min/mg) <11.6 (0.1) 28.2 (0.5) <11.6 (0.2) <11.6 (0.7)
Hepatocyte CLint (μl/min/106 cells)b <2 9 4 <4
Hepatocyte predicted EHb <0.2 0.65 0.23 <0.2
fu microsomes 0.15 (0.01) 0.50 (0.04) 0.45 (0.05) 0.47 (0.04)
fu plasma 0.17 (0.009) 0.10 (0.007) 0.15 (0.009) 0.10 (0.02)
Blood/plasma ratio 1.5 (0.1) 2.3 (0.1) 2.1 (0.2) 1.9 (0.2)
Plasma stability (after 240 min) (%)b 97 95 97 102
a

Permeability across Caco-2 cells in both directions, Papp B→A and Papp A→B, was determined as (25 ± 5) × 10−6 cm/s and (28 ± 2) × 10−6 cm/s, respectively.

b

Single determination.