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Diltiazem

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	Diltiazem	15.8		1-methyl-4-phenylpyridinium (MPP+)	HEK293-OCT1	Umehara, 2008
SLC22A1	OCT1	Diltiazem	1.7		1-methyl-4-phenylpyridinium (MPP+)	MDCK-OCT1	Grube, 2011
SLC22A1	OCT1	Diltiazem	12.4		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Ahlin, 2008
ABCB1	MDR1, P-gp	Diltiazem	42.7		Calcein AM	MDR1 expressing A2780/ADR cells	Muller, 2007
ABCB1	MDR1, P-gp	Diltiazem	49		Calcein AM	MDR1 expressing A2780/ADR cells	Klinkhammer, 2009
ABCB1	MDR1, P-gp	Diltiazem	77.7		Digoxin	MDR1 expressing LLC-PK1 cells	Takara, 2002
ABCC2	MRP2, cMOAT	Diltiazem	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Diltiazem	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Diltiazem	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCB1	MDR1, P-gp	Diltiazem	42.7		Hoechst 33342	MDR1 expressing A2780/ADR cells	Pick, 2008
ABCB11	BSEP	Diltiazem	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC47A1	MATE1	Diltiazem		12.5	Tetraethylammonium	HEK293-MATE1	Tsuda, 2009
SLC47A2	MATE2K	Diltiazem		117	Tetraethylammonium	HEK293-MATE2	Tsuda, 2009
SLC22A4	OCTN1	Diltiazem	126.4		Tetraethylammonium	MDCKII-hOCTN1	Grube, 2011

No drug-drug interaction information.