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. Author manuscript; available in PMC: 2022 Nov 21.
Published in final edited form as: J Med Chem. 2020 Jan 24;63(3):1298–1312. doi: 10.1021/acs.jmedchem.9b01769

Table 7.

Human Microsomal Stability of 24b and 25b.

Compound Human Liver Microsome
R2 T1/2 (min) CLint(mic)
(μL/min/mg)
CLint(liver)
(mL/min/kg)
Remaining
(T=60min)
24b 0.9412 80.1 17.3 15.6 55.8%
25b 0.9322 32.7 42.4 38.2 23.8%
K-5a2 0.9973 2.4 577.3 519.6 0.8%
25a 0.992 1.6 847.3 762.5 0.2%
Propafenone 0.9846 5.2 265.9 239.3 0.1%

R2 is the correlation coefficient of the linear regression for the determination of kinetic constant

CLint(mic) = 0.693/half-life/mg microsome protein per mL

CLint (liver) = CLint (mic)*mg microsomal protein/g liver weight*g liver weight/kg body weight

Liver weight: 20 g/kg for human.