Evaluating Hepatobiliary Transport with ¹⁸F-Labeled Bile Acids: The Effect of Radiolabel Position and Bile Acid Structure on Radiosynthesis and In Vitro and In Vivo Performance

Table 2

Calculated Ki-values of the bile acid analogues for NTCP, OATP1B1, and BSEP. Data are mean ± SD (n = 3). 3βFCA IC50-values were extracted from literature [13] and used to calculate the Ki-values.

	Ki for NTCP (µM)	Ki for OATP1B1 (µM)	Ki for BSEP (µM)
CA	12.96 ± 4.26	42.70 ± 0.16	95.46 ± 33.97
3αFCA	2.53 ± 0.76	5.22 ± 0.56	198.93 ± 39.47
3βFCA	6.18 ± 0.59	9.67 ± 0.83	216.30 ± 52.99
3βFGCA	1.09 ± 0.34	4.24 ± 0.16	87.38 ± 14.61
3βFCDCA	0.91 ± 0.02	0.64 ± 0.07	48.24 ± 3.94
12βFCA	30.08 ± 9.40	4.56 ± 0.25	367.02 ± 38.11