TABLE 2

Pharmacokinetic parameters of blebbistatin, NBleb, and AmBleb from experiments using rat and human hepatocytes

Clint = (ln2/t1/2) × ((cell number/tissue weight)/(cell number/incubation volume)) × (liver weight/body weight), where t1/2 is the time required to achieve 50% of the initial concentration at t = 0 min. ClH = (Clint × fu × HPF)/(Clint × fu + HPF), where HPF = QH × plasma/blood ratio, where QH = 55.2 ml/min per kilogram for rat, 20.7 ml/min per kilogram for human, plasma/blood ratio = 0.63 for rat, 0.57 for human. EH = ClH/QH. F (bioavailability) = 100*(1−EH).

Substancet1/2 (min)Clint (ml/min per kilogram)ClH (ml/min per kilogram)EHF (%)
Rat
Blebbistatin20.1780.4122.620.4159.02
NBleb114.3014.1910.080.1881.74
AmBleb18.9885.4624.080.4456.38
Human
Blebbistatin26.1343.728.840.4357.31
NBleb20.3156.259.750.4752.88
AmBleb52.1521.917.430.3664.11