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Sildenafil

In Vitro Substrates

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

Transporter	Synonyms	Km (μM)	Cell System	Reference
ABCG2	BCRP, MXR	22.4	MDCK-transfected cells	Choi, 2012

* 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
ABCC5	MRP5	Sildenafil	580		5-fluorodeoxyuridine monophosphate	MRP5-expressing HEK293 vesicles	Pratt, 2005
ABCC4	MRP4	Sildenafil	20		9-(2-phosphonomethoxyethyl)adenine (PMEA)	MRP4-expressing HEK293 vesicles	Reid, 2003
ABCC5	MRP5	Sildenafil	80		9-(2-phosphonomethoxyethyl)adenine (PMEA)	MRP4-expressing HEK293 vesicles	Reid, 2003
SLCO1B1	OATP1B1, OATP-C, OATP2, LST-1	Sildenafil	1.5		Bosentan	CHO-OATP1B1	Treiber, 2007
SLCO1B3	OATP1B3, OATP8	Sildenafil	0.8		Bosentan	CHO-OATP1B1	Treiber, 2007
ABCG2	BCRP, MXR	Sildenafil	3.1		Cholecystokinin octapeptide	BCRP membrane vesicles	Yee, 2021
ABCC5	MRP5	Sildenafil		0.267	Cyclic GMP	MRP5-expressing V79 vesicles	Jedlitschky, 2000
SLC22A8	OAT3	Sildenafil		20.5	Estrone sulfate	HEK293-OAT3	Yee, 2021
SLC22A1	OCT1	Sildenafil	19.8		Metformin	HEK293-OCT1	Yee, 2021

No drug-drug interaction information.