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SLC22A5

Synonyms: CDSP, FLJ46769, OCTN2, OCTN2VT

Entrez Gene Link

Expression Data
Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

Expression Data

Expression data for other tissues could be found in http://pharmacogenetics.ucsf.edu/gtex/index.html

Asterisk indicates important transporters in the organ as identified in the organ diagram.

Organ Source Relative Expression
Brain Nishimura    0.00435
Kidney* Nishimura    0.0511
Liver* Nishimura    0.00248
Placenta* Nishimura    0.0338
Small Intestine* Nishimura    0.0136
Kidney* Mean across all PMT Samples 11.276
Liver* Mean across all PMT Samples 1.562
Note that relative expression values should only be compared between entries of the same source.

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In Vitro Substrates

Substrate Km (μM) Cell System Reference
Acetyl-L-carnitine 8.5 HEK293-OCTN2 Ohashi, 1999
Acetyl-L-carnitine 6.57 primary epididymal spermatozoa Kobayashi, 2007
Acetyl-L-carnitine 26 TR-iBRB2 cells Tachikawa, 2010
Amisulpride 185 HEK293-hOCTN2 Dos, 2014
Cephaloridine 3000 hOCTN2-expressing oocytes Kano, 2009
D-carnitine 10.9 HEK293-OCTN2 Ohashi, 1999
D-carnitine 98.3 OCTN2-expressing oocytes Wagner, 2000
Ethambutol 455 HEK293-hOCTN2 Parvez, 2018
Etoposide 150 LLC-PK1-hOCTN2 Hu, 2012
Ipratropium 53 HEK293-OCTN2 Nakamura, 2010
L-carnitine 4.3 HEK293-OCTN2 Ohashi, 1999
L-carnitine 3.5 HeLa-OCTN2 Ganapathy, 2000
L-carnitine 4.8 OCTN2-expressing oocytes Wagner, 2000
L-carnitine 23.6 primary epididymal spermatozoa Kobayashi, 2007
L-carnitine 29 TR-iBRB2 cells Tachikawa, 2010
Mildronate 26 HEK293-hOCTN2 Grigat, 2009
Pivaloylcarnitine 166 HEK293-hOCTN2 Ohnishi, 2008
Quinidine ND HEK293-OCTN2 Ohashi, 1999
Sulpiride 235 MDCK-hOCTN2 Li, 2017
Tetraethylammonium 63 HRPE-hOCTN2 Wu, 1999
Tetraethylammonium 215.7 HEK293-hOCTN2 Tamai, 2000
Valproylcarnitine 168 HEK293-hOCTN2 Ohnishi, 2008
Verapamil ND HEK293-OCTN2 Ohashi, 1999

ND = not determined
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022


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In Vitro Inhibitors

Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
1-methyl-4-phenylpyridinium (MPP+) 1700 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Acetyl-DL-carnitine 15.7 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Acyclovir 5130 L-carnitine MDCKII-hOCTN2 Diao, 2009
Amiodarone 5.72 L-carnitine MDCKII-hOCTN2 Diao, 2009
Amlodipine 96 L-carnitine MDCKII-hOCTN2 Diao, 2009
Amphetamine 6000 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Atenolol 8000 L-carnitine MDCKII-hOCTN2 Diao, 2009
Atropine 4000 L-carnitine MDCKII-hOCTN2 Diao, 2009
Bromocriptine 16.6 L-carnitine MDCKII-hOCTN2 Diao, 2009
Carvedilol 10.7 L-carnitine MDCKII-hOCTN2 Diao, 2009
Cediranib 2.49 L-carnitine HEK293-hOCTN2 Johnston, 2014
Cefazolin 6740 L-carnitine L6-hOCTN2 Todesco, 2008
Cefepime 1000 L-carnitine JAR-hOCTN2 Ganapathy, 2000
Cefepime 1700 L-carnitine HeLa-OCTN2 Ganapathy, 2000
Cefoselis 6400 L-carnitine HeLa-OCTN2 Ganapathy, 2000
Cefuroxime 525 L-carnitine L6-hOCTN2 Todesco, 2008
Cephalexin 3037 L-carnitine L6-hOCTN2 Todesco, 2008
Cephaloridine 180 L-carnitine JAR-hOCTN2 Ganapathy, 2000
Cephaloridine 230 L-carnitine HeLa-OCTN2 Ganapathy, 2000
Cephaloridine 379 L-carnitine MDCKII-hOCTN2 Diao, 2010
Cerivastatin 425 L-carnitine MDCKII-hOCTN2 Diao, 2009
Cetirizine 79.8 L-carnitine MDCKII-hOCTN2 Diao, 2010
Chloroephedrine 4800 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Cisapride 66.7 L-carnitine MDCKII-hOCTN2 Diao, 2010
Clozapine 47.3 L-carnitine MDCKII-hOCTN2 Diao, 2009
D-carnitine 16.5 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Daunorubicin 502 L-carnitine MDCKII-hOCTN2 Diao, 2010
Desloratadine 53.3 L-carnitine MDCKII-hOCTN2 Diao, 2009
Duloxetine 118 L-carnitine MDCKII-hOCTN2 Diao, 2009
Emetine 4.2 L-carnitine OCTN2-expressing oocytes Wagner, 2000
Ephedrine 2700 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Erythromycin 2870 L-carnitine MDCKII-hOCTN2 Diao, 2009
Erythromycin 2870 L-carnitine MDCKII-hOCTN2 Diao, 2010
Etoposide 55 L-carnitine LLC-PK1-hOCTN2 Hu, 2012
Ezetimibe 29.3 L-carnitine MDCKII-hOCTN2 Diao, 2010
Furosemide 1350 L-carnitine MDCKII-hOCTN2 Diao, 2010
Gabapentin 1700 L-carnitine MDCKII-hOCTN2 Diao, 2010
Gefitinib 29 L-carnitine MDCKII-hOCTN2 Diao, 2009
Grepafloxacin 1000 L-carnitine Caco-2 cells expressing OCTN2 Hirano, 2006
Grepafloxacin 300 L-carnitine BeWo cells expressing OCTN2 Hirano, 2008
Hydrochlorothiazide 4110 L-carnitine MDCKII-hOCTN2 Diao, 2009
Irinotecan 219 L-carnitine MDCKII-hOCTN2 Diao, 2010
Ketorolac 1530 L-carnitine MDCKII-hOCTN2 Diao, 2009
Ketorolac 1530 L-carnitine MDCKII-hOCTN2 Diao, 2010
L-carnitine 11.8 L-carnitine HRPE-hOCTN2 Wu, 1999
L-carnitine 3.7 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Lamivudine 2590 L-carnitine MDCKII-hOCTN2 Diao, 2009
Lamivudine 2590 L-carnitine MDCKII-hOCTN2 Diao, 2010
Levofloxacin 6800 L-carnitine Caco-2 cells expressing OCTN2 Hirano, 2006
Levofloxacin 3000 L-carnitine BeWo cells expressing OCTN2 Hirano, 2008
Levofloxacin 1900 L-carnitine MDCKII-hOCTN2 Diao, 2009
Levofloxacin 1890 L-carnitine MDCKII-hOCTN2 Diao, 2010
Lomefloxacin 4000 L-carnitine MDCKII-hOCTN2 Diao, 2009
Metformin 2050 L-carnitine MDCKII-hOCTN2 Diao, 2010
Methamphetamine 2300 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Mildronate 26.1 L-carnitine MDCKII-hOCTN2 Grube, 2006
Nelfinavir 29.2 L-carnitine MDCKII-hOCTN2 Diao, 2009
Nifedipine 59.4 L-carnitine MDCKII-hOCTN2 Grube, 2011
Nizatidine 183 L-carnitine MDCKII-hOCTN2 Diao, 2010
Nor-psi-ephedrine 9200 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Norephedrine 7100 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Omeprazole 5.2 L-carnitine hOCTN2-reconstituted proteoliposomes Pochini, 2009
Penfluridol 26.5 L-carnitine MDCKII-hOCTN2 Diao, 2010
Procainamide 1400 L-carnitine MDCKII-hOCTN2 Diao, 2010
Procarbazine 2520 L-carnitine MDCKII-hOCTN2 Diao, 2009
Procarbazine 2520 L-carnitine MDCKII-hOCTN2 Diao, 2010
Prochlorperazine 51.3 L-carnitine MDCKII-hOCTN2 Diao, 2009
Progesterone 48.6 L-carnitine BeWo cells expressing OCTN2 Rytting, 2008
Propafenone 74.2 L-carnitine MDCKII-hOCTN2 Diao, 2010
Propantheline 20.4 L-carnitine MDCKII-hOCTN2 Diao, 2009
Psi-ephedrine 4200 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Pyrilamine 41.7 L-carnitine HEK293-hOCTN2 Kobayashi, 2007
Quinidine 239 L-carnitine HEK293-hOCTN2 Kobayashi, 2007
Raloxifene 13.8 L-carnitine MDCKII-hOCTN2 Diao, 2009
Reserpine 32.2 L-carnitine MDCKII-hOCTN2 Diao, 2010
Rifampin 1150 L-carnitine MDCKII-hOCTN2 Diao, 2009
Risperidone 114 L-carnitine MDCKII-hOCTN2 Diao, 2010
Ritonavir 7.73 L-carnitine MDCKII-hOCTN2 Diao, 2010
Roxithromycin 333 L-carnitine MDCKII-hOCTN2 Diao, 2010
Selegiline 1230 L-carnitine MDCKII-hOCTN2 Diao, 2009
Simvastatin 12.4 L-carnitine MDCKII-hOCTN2 Diao, 2010
Sodium valproate 2600 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Spironolactone 36 L-carnitine MDCKII-hOCTN2 Grube, 2011
Succinylcholine 2700 L-carnitine MDCKII-hOCTN2 Diao, 2009
Succinylcholine 2700 L-carnitine MDCKII-hOCTN2 Diao, 2010
Tamoxifen 20 L-carnitine MDCKII-hOCTN2 Diao, 2009
Tetraethylammonium 80 L-carnitine HRPE-hOCTN2 Wu, 1999
Tetraethylammonium 1200 L-carnitine BeWo cells expressing OCTN2 Rytting, 2005
Tetraethylammonium 132 L-carnitine HEK293-hOCTN2 Kobayashi, 2007
Thioridazine 23 L-carnitine MDCKII-hOCTN2 Diao, 2009
Thioridazine 1.06 L-carnitine MDCKII-hOCTN2 Jiang, 2019
Trifluoperazine 67.3 L-carnitine MDCKII-hOCTN2 Diao, 2009
Verapamil 21.4 Ethambutol HEK293-hOCTN2 Parvez, 2018
Verapamil 58.8 L-carnitine HEK293-hOCTN2 Kobayashi, 2007
Verapamil 5.3 L-carnitine L6-hOCTN2 Todesco, 2008
Verapamil 17.6 L-carnitine MDCKII-hOCTN2 Diao, 2009
Verapamil 50.9 L-carnitine MDCKII-hOCTN2 Grube, 2011
Vinblastine 4.85 L-carnitine MDCKII-hOCTN2 Diao, 2009
Vincristine 15.9 L-carnitine MDCKII-hOCTN2 Diao, 2010
Vinorelbine 26.8 L-carnitine MDCKII-hOCTN2 Diao, 2010
Zidovudine 2140 L-carnitine MDCKII-hOCTN2 Diao, 2009
Zidovudine 2140 L-carnitine MDCKII-hOCTN2 Diao, 2010

ND = not determined
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022


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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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