TABLE 1

Bidirectional transepithelial transport of Exp3174 in Caco-2 cells

The subscripts A, B, and C represent apical side, basolateral side, and cell lysate, respectively. Data are shown as the mean ± S.D. (n = 3).

	Exp3174	Exp3174 Dosing Concentration
	(nM)	2 μM	10 μM	50 μM
A to B	C_0, A	1937 ± 107	9267 ± 286	44,367 ± 2212
	C_2h, A	1953 ± 59	9690 ± 282	45,033 ± 2363
	C_2h, B	BQL	BQL	1.43 ± 0.06
	C_2h, C	2.32 ± 0.21	10.0 ± 0.8	49.0 ± 0.5
	P_{app,A to B} (×10⁻⁸ cm/s)	2.50 ± 0.1^{^a}	1.64 ± 0.0^{^a}	1.56 ± 0.0
B to A	C_0, B	1973 ± 105	9620 ± 358	44,733 ± 1002
	C_2h, B	1863 ± 97	9723 ± 195	45,367 ± 2593
	C_2h, A	7.97 ± 0.39	38.3 ± 4.3	235 ± 20
	C_2h, C	19.3 ± 0.2	100 ± 14	328 ± 11
	P_{app,B to A} (×10⁻⁸ cm/s)	25.6 ± 2.1	25.1 ± 2.6	33.2 ± 3.6
	ER	10.2^{^a}	15.3^{^a}	21.2

↵^a P_app was calculated based on the lower limit of quantitation (0.2 nM), as the concentration of Exp3174 in receiver side was below the quantitation limit (BQL), and thereby the calculated ER values were only for reference.