TABLE 3

Probe substrates and substrate concentrations used to characterize the rates and routes of metabolism in human freshly isolated lung parenchymal cells and human pooled cryopreserved hepatocytes

Rate concentrations were carried out at 1 μm and 2 μm in hepatocytes and LPCs, respectively.


Substrate

Rate Incubations in Hepatocytes

Rate Incubations in LPCs

Route Incubations in Hepatocytes and LPCs

Km of Reactiona
μM μM
7-EC 1 2 25 3.9 μM (1)
ER 1 2 20 0.18-0.21 μM (2)
Coumarin 1 2 25 0.3-2.3 μM (2)
Bupropion 1 2 50 67-168 μM (2)
Diclofenac 1 2 50 3.4-52 μM (2)
S-Mephenytoin 1 2 100 13-35 μM (2)
Bufuralol 1 2 20 9-15 μM (2)
Astemizole 1 2 50 1.8 μM (3)
Midazolam 1 2 25 1-14 μM (2)
Testosterone 1 2 100 52-94 μM (2)
7-HC 1 2 25 UGT 79 μM (4)
SULT ~3 μM (4)
1-Naphthol 1 2 25 40.2 μM (5)
4-methyl umbelliferone 1 2 25 920 μM (6)
Acetaminophen 1 2 25 UGT 2.2 mM (7)
SULT <1 mM (8)
BDP 1 2 50
Salbutamol 1 2 25 142 μM (9)
Budesonide 1 2 25 126.9 μM (10)
Formoterol
1
2
25
827.6 μM (11)