Table 1

Affinities for inhibition of NTCP-mediated taurocholate uptake by bile acids, organic anion (bromosulfophthalein), and drugs

InhibitorIC50
μM
Cyclosporin1.0
Ursodeoxycholic acid3.6
Cholic acid5.3
(R)-Propranolol5.5
(S)-Propranolol6.1
Bromosulfophthalein7.3
Furosemide15
Ketoconazole264

Values are inhibitory constant, IC50, derived from studies (n = 3) carried out on 3 or more study days.