Table 1.
Compound | Media | Plasma binding (%) | k (h−1) | t1/2(h) | r2 |
---|---|---|---|---|---|
CO-103 | SIF (2% Kolliphor) | 0.357 ± 0.036 | 1.93 ± 0.18 | 0.989 | |
SIF (50% DMSO) | 1.644 ± 0.027 | 0.42 ± 0.01 | 0.998 | ||
Plasma | 92 ± 1 | 0.541 ± 0.05 | 1.29 ± 0.12 | 0.99 | |
CO-104 | SIF (2% Kolliphor) | 0.036 ± 0.006 | 17.56 ± 0.82 | 0.991 | |
SIF (50% DMSO) | 0.165 ± 0.013 | 4.22 ± 0.33 | 0.984 | ||
Plasma | 91 ± 1 | 0.116 ± 0.002 | 5.99 ± 0.11 | 0.997 | |
CO-125 | SIF (2% Kolliphor) | 0.297 ± 0.041 | 2.33 ± 0.21 | 0.991 | |
SIF (50% DMSO) | 0.926 ± 0.038 | 0.75 ± 0.03 | 0.986 | ||
Plasma | 90 ± 2 | 0.476 ± 0.016 | 1.55 ± 0.05 | 0.995 | |
CO-115 | SIF (2% Kolliphor) | 0.152 ± 0.013 | 4.85 ± 0.35 | 0.997 | |
SIF (50% DMSO) | 0.109 ± 0.008 | 6.39 ± 0.46 | 0.993 | ||
Plasma | 84 ± 1 | 0.136 ± 0.007 | 5.11 ± 0.26 | 0.988 | |
CO-116 | SIF (2% Kolliphor) | 0.401 ± 0.075 | 1.82 ± 0.15 | 0.997 | |
SIF (50% DMSO) | 0.384 ± 0.025 | 1.58 ± 0.12 | 0.994 | ||
Plasma | 84 ± 2 | 0.473 ± 0.051 | 1.48 ± 0.16 | 0.978 |
k: first-order rate constant for the conversion reactions of prodrugs; t1/2: conversion half-life for the conversion reactions of prodrugs; r2: measure of the goodness of fit for the nonlinear regression; Results are presented as the mean ± SD (n ≥ 3).