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Carvedilol

In Vitro Substrates

No substrate information.

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter

Transporter	Synonyms	Inhibitor	IC50 (μM)	Ki (μM)	Substrate used	Cell System	Reference
SLC22A1	OCT1	Carvedilol	1.4		1-methyl-4-phenylpyridinium (MPP+)	MDCK-OCT1	Grube, 2011
SLC22A2	OCT2	Carvedilol	55.2		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Belzer, 2013
SLC47A1	MATE1	Carvedilol	92.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-MATE1	Wittwer, 2013
SLC22A1	OCT1	Carvedilol	3.43		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Chen, 2017
ABCB1	MDR1, P-gp	Carvedilol	4.6		Daunorubicin	NIH-3T3-G185 cells	Wang, 2001
ABCC2	MRP2, cMOAT	Carvedilol	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Carvedilol	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Carvedilol	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A5	OCTN2	Carvedilol		10.7	L-carnitine	MDCKII-hOCTN2	Diao, 2009
ABCB1	MDR1, P-gp	Carvedilol	6		LDS-751	NIH-3T3-G185 cells	Wang, 2001
SLC22A2	OCT2	Carvedilol	63		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
SLC22A2	OCT2	Carvedilol	13.1		NBD-MTMA	CHO-OCT2	Belzer, 2013
ABCB1	MDR1, P-gp	Carvedilol	6.6		Rhodamine 123	NIH-3T3-G185 cells	Wang, 2001
ABCB11	BSEP	Carvedilol	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A4	OCTN1	Carvedilol	73.1		Tetraethylammonium	MDCKII-hOCTN1	Grube, 2011

No drug-drug interaction information.