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SLC22A11

Synonyms: MGC34282, OAT4, hOAT4

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 BLQ
Kidney* Nishimura    0.125
Liver Nishimura BLQ
Placenta* Nishimura    0.106
Small Intestine Nishimura BLQ
Kidney* Mean across all PMT Samples 12.708
Liver Mean across all PMT Samples BLQ
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
Bumetanide 306 S2-OAT4 Hasannejad, 2004
Dehydroepiandrosterone sulfate 0.63 OAT4-expressing oocytes Cha, 2000
Estrone sulfate 1.01 OAT4-expressing oocytes Cha, 2000
Estrone sulfate 9.9 S2-OAT4 Takeda, 2002
Estrone sulfate 38.1 CHO cells Yang, 2010
Methotrexate 17.8 S2-OAT4 Takeda, 2002
Ochratoxin A 22.9 S2-OAT4 Babu, 2002
Pravastatin 257 S2-OAT4 Nakagomi-Hagihara, 2007
Prostaglandin E2 0.154 S2-OAT4 Kimura, 2002
Prostaglandin F2-alpha 0.692 S2-OAT4 Kimura, 2002
Tetracycline 122.7 S2-OAT4 Babu, 2002
Uric acid 106 HEK293-OAT4 Sato, 2008
Zidovudine 152 S2-OAT4 Takeda, 2002

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
Acetazolamide 425 Estrone sulfate S2-OAT4 Hasannejad, 2004
Alpha-zearalenol 130 Estrone sulfate S2 cells Tachampa, 2008
Aristolochic acid I - 20.5 Estrone sulfate HEK293 cells Bakhiya, 2009
Betamipron 502 Prostaglandin F2-alpha S2-OAT4 Enomoto, 2002
Bumetanide 348 Estrone sulfate S2-OAT4 Hasannejad, 2004
Candesartan 60 Uric acid HEK293-OAT4 Sato, 2008
Cefamandole 1140 Prostaglandin F2-alpha S2-OAT4 Khamdang, 2003
Cefazolin 1740 Prostaglandin F2-alpha S2-OAT4 Khamdang, 2003
Cefoperazone 2800 Prostaglandin F2-alpha S2-OAT4 Khamdang, 2003
Cefotaxime 6150 Prostaglandin F2-alpha S2-OAT4 Khamdang, 2003
Ceftriaxone 2380 Prostaglandin F2-alpha S2-OAT4 Khamdang, 2003
Cephaloridine 3630 Prostaglandin F2-alpha S2-OAT4 Khamdang, 2003
Cephalothin 200 Prostaglandin F2-alpha S2-OAT4 Khamdang, 2003
Chlorothiazide 2632 Estrone sulfate S2-OAT4 Hasannejad, 2004
Citreoviridin A 823 Estrone sulfate S2 cells Tachampa, 2008
Citrinin 366.4 Ochratoxin A S2-OAT4 Babu, 2002
Cyclopiazonic acid 86.6 Estrone sulfate S2 cells Tachampa, 2008
Diclofenac 34.5 Estrone sulfate S2-OAT4 Khamdang, 2002
Ethacrynic acid 8.76 Estrone sulfate S2-OAT4 Hasannejad, 2004
Furosemide 44.5 Estrone sulfate S2-OAT4 Hasannejad, 2004
Ibuprofen 103 Estrone sulfate S2-OAT4 Khamdang, 2002
Indomethacin 10.1 Estrone sulfate S2-OAT4 Khamdang, 2002
Ketoprofen 70.3 Estrone sulfate S2-OAT4 Khamdang, 2002
KW-3902 20.7 Prostaglandin F2-alpha S2-OAT4 Enomoto, 2002
Losartan 18 Uric acid HEK293-OAT4 Sato, 2008
Mefenamic acid 61.7 Estrone sulfate S2-OAT4 Khamdang, 2002
Naproxen 85.4 Estrone sulfate S2-OAT4 Khamdang, 2002
Novobiocin 92.68 90.5 Estrone sulfate COS7-OAT4 Duan, 2009
Octanoate 235.5 Ochratoxin A S2-OAT4 Babu, 2002
Olmesartan 4.4 Uric acid HEK293-OAT4 Sato, 2008
Piroxicam 84.9 Estrone sulfate S2-OAT4 Khamdang, 2002
Piroxicam 107.8 Ochratoxin A S2-OAT4 Babu, 2002
Pratosartan 31 Uric acid HEK293-OAT4 Sato, 2008
Probenecid 44.4 Ochratoxin A S2-OAT4 Babu, 2002
Probenecid 54.9 Prostaglandin F2-alpha S2-OAT4 Enomoto, 2002
Sulindac 617 Estrone sulfate S2-OAT4 Khamdang, 2002
Telmisartan 1.2 Uric acid HEK293-OAT4 Sato, 2008
Trichlormethiazide 1505 Estrone sulfate S2-OAT4 Hasannejad, 2004
Valsartan 26 Uric acid HEK293-OAT4 Sato, 2008

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

DDI Implicated Transporter Interacting Drug Affected Drug AUC Cmax CLR CL/F t1/2 Effect on PD Reference More Details
Clinical PK Impact(fold change)
1 OATs/OCTs Cotrimoxazole (trimethoprim/sulfamethoxazole) Apricitabine 1.7 1.3 0.6 0.6 1.4 ND Shiveley, 2008 DDI 1
2 OATs/OCTs Cotrimoxazole (trimethoprim/sulfamethoxazole) Zidovudine NS ND 0.4 NS NS ND Chatton, 1992 DDI 2
3 OATs Furosemide Lomefloxacin 1.1 NS 0.7 0.9 NS ND Sudoh, 1994 DDI 3
4 OATs Probenecid Acyclovir 1.4 ND 0.7 NS ND ND Laskin, 1982 DDI 4
5 OATs Probenecid Cefaclor 2.1 1.5 ND ND 1.6 ND Welling, 1979 DDI 5
6 OATs Probenecid Cefonicid 2.1 1.2 0.3 ND 1.5 ND Pitkin, 1981 DDI 6
7 OATs Probenecid Cefoxitin 2.4 ND 0.4 ND 2.0 ND Vlasses, 1980 DDI 7
8 OATs Probenecid Ceftriaxone 0.7 ND ND 1.3 0.8 ND Stoeckel, 1988 DDI 8
9 OATs Probenecid Cephradine 2.4 1.9 ND ND 1.5 ND Welling, 1979 DDI 9
10 OATs Probenecid Cidofovir ND ND 0.5 0.6 ND ND Cundy, 1995 DDI 10
11 OATs/MRPs Probenecid Ciprofloxacin 1.7 NS 0.4 0.6 1.5 ND Jaehde, 1995 DDI 11
12 OATs Probenecid Dicloxacillin 1.9 1.8 0.3 0.5 ND ND Beringer, 2008 DDI 12
13 OATs Probenecid Famotidine 1.8 1.5 0.4 0.1 NS ND Inotsume, 1990 DDI 13
14 OATs/MRPs Probenecid Furosemide 2.7 1.5 0.3 0.4 1.7 ND Vree, 1995 DDI 14

The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PK = pharmacokinetic
PD = pharmacodynamic
ND = not determined
NS = not significant
N/A = information not available
Calculation of Fold Change: fold change in the presence of the interacting drug = (value with interacting drug)/(value without interacting drug)
fold change > 1: increase in pharmacokinetic value
fold change < 1: decrease in pharmacokinetic value
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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