Table 1.

The results of iruplinalkib as P-gp and BCRP substrate, BCRP and P-gp inhibitor investigation

Potential ABC transporters on Caco-2 cells	Reference inhibitors		Standard or examination substrate		Exhaust Ratio			Exhaust inhibition rate (%)
	Compound	Conc (µM)	Compound	Conc (µM)	Mean	SD	CV (%)
P-gp			Digoxin	5	161.2	42.98	26.7
	Elacridar	10			0.688	0.220	32.0	99.6
	Verapamil	50			3.349	0.041	1.24	97.9
BCRP			E3S	10	20.54	5.218	25.4
	Elacridar	10			1.715	0.253	14.7	91.7
	Ko143	10			2.816	0.599	21.3	86.3
P-gp/BCRP/MRP2			Iruplinalkib	0.5	20.34	4.965	24.4
	Elacridar	10			2.808	0.261	9.29	86.2
	Verapamil	50			3.456	0.659	19.1	83.0
	Ko143	10			20.95	4.181	20.0	-3.0
				5	84.23	12.71	15.1
	Elacridar	10			0.605	0.197	32.5	99.3
	Verapamil	50			2.626	0.165	6.28	96.9
	Ko143	10			26.14	6.666	25.5	69.0
				50	8.020	1.399	17.4
	Elacridar	10			0.614	0.130	21.2	92.3
	Verapamil	50			1.954	0.107	5.49	75.6
	Ko143	10			9.889	3.193	32.3	-23.3
BCRP			E3S	10	20.54	5.218	25.4
	Elacridar	10			1.715	0.253	14.7	91.6
	Ko143	10			2.816	0.599	21.3	86.3
	Iruplinalkib	30			15.13	3.542	23.4	26.3
		10			0.570	0.024	4.14	97.2
		3			10.09	1.418	14.1	50.9
		1			18.84	4.401	23.4	8.3
		0.3			12.79	2.246	17.6	37.7
		0.1			22.82	3.758	16.5	-11.1
P-gp			Digoxin	5	161.2	42.98	26.7
	Elacridar	10			0.688	0.220	32.0	99.6
	Verapamil	10			3.349	0.041	1.24	97.9
	Iruplinalkib	30			2.165	0.479	22.1	98.7
		10			16.44	3.174	19.3	89.8
		3			191.9	33.67	17.5	-19.1
		1			182.4	24.32	13.3	-13.2
		0.3			154.8	6.244	4.03	3.97
		0.1			210.9	29.16	13.8	-30.9

Note: ABC, adenosine triphosphate binding cassette; SD, standard deviation; CV, coefficient of variation