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. 2023 Mar 6;66(6):3968–3994. doi: 10.1021/acs.jmedchem.2c01905

Table 3. In Vitro Metabolic Stability of 7aa.

mouse hepatocytes
in vitro t1/2 [min] 160
Clint [μL/106 cells/min] 9.0
Clint (pred. in vivo) [mL/min] 2.1
ClH (pred.) [mL/min] 0.05
Epred 0.03
mouse liver microsomes
in vitro t1/2 [min] 87
Clint [μL/106 cells/min] 16
Clint (pred. in vivo) [mL/min] 1.3
ClH (pred.) [mL/min] 0.03
Epred 0.01
human liver microsomes
in vitro t1/2 [min] 103
Clint [μL/106 cells/min] 13
Clint (pred. in vivo) [mL/min] 630
ClH (pred.) [mL/min] 14
Epred 0.01
a

Abbreviations: t1/2, elimination half-life; Clint, intrinsic clearance; ClH, hepatic clearance; Epred, predicted hepatic extraction ratio (the fraction of drug removed from blood by the liver in one passage); and pred., predicted.