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SLC22A8

Synonyms: MGC24086, OAT3

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    0.000504
Kidney* Nishimura    0.818
Liver Nishimura    0.000135
Placenta Nishimura BLQ
Small Intestine Nishimura BLQ
Kidney* Mean across all PMT Samples   17.974
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

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Substrate Km (μM) Cell System Reference
Bumetanide* 1586 S2-OAT3 Hasannejad, 2004
Cefaclor ND HEK293-OAT3 Ueo, 2005
Ceftizoxime ND HEK293-OAT3 Ueo, 2005
Cimetidine 113 HEK293-OAT3 Tahara, 2006
Cimetidine 174 CHO-OAT3 Chu, 2007
Cimetidine 57.4 OAT3-expressing oocytes Cha, 2001
Cortisol 2.4 OAT3-expressing oocytes Asif, 2005
Dimesna 390 HeLa-OAT3 Cutler, 2012
Edaravone sulfate 15.1 HEK293-OAT3 Mizuno, 2007
Estrone 3-sulfate 2.18 COS7-OAT3 Duan, 2009
Estrone 3-sulfate 2.21 S2-OAT3 Takeda, 2001
Estrone 3-sulfate 3.1 OAT3-expressing oocytes Cha, 2001
Estrone 3-sulfate 6.3 HEK293-OAT3 Ueo, 2005
Estrone 3-sulfate 7.5 S2-OAT3 Takeda, 2000
Fexofenadine 70.2 HEK293-OAT3 Tahara, 2006
Furosemide* ND S2-OAT3 Hasannejad, 2004
Methotrexate 10.9 OAT3-expressing oocytes Cha, 2001
Methotrexate 17.2 OAT3-expressing oocytes Uwai, 2004
Methotrexate 21.1 S2-OAT3 Takeda, 2002
Ochratoxin A 0.75 S2-OAT3 Jung, 2001
Olmesartan 0.12 HEK293-OAT3 Yamada, 2007
Para-aminohippurate 87.2 OAT3-expressing oocytes Cha, 2001
Pitavastatin 3.3 OAT3-expressing oocytes Fujino, 2005
Pravastatin 27.2 S2-OAT3 Nakagomi-Hagihara, 2007
Prostaglandin E2 0.345 S2-OAT3 Kimura, 2002
Prostaglandin F2alpha 1.092 S2-OAT3 Kimura, 2002
Rosuvastatin 7.4 OAT3-expressing oocytes Windass, 2007
Sitagliptin 162 CHO-OAT3 Chu, 2007
Tetracycline 566.2 S2-OAT3 Babu, 2002
Uric acid 380.3 HEK293-OAT3 Sato, 2008
Zidovudine 145 S2-OAT3 Takeda, 2002

ND = not determined


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In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
(Noradamantan-3-yl)-1,3-dipropylxanthine (KW-3902) 3.7 Estrone 3-sulfate S2-OAT3 Takeda, 2001
1-butanesulfonic acid (BSA) 5098 Estrone 3-sulfate CHO-OAT3 Astorga, 2011
2,3-Dimercapto-1-propane sulfonate (DMPS) 40 Estrone 3-sulfate CHO-OAT3 Astorga, 2011
3-mercapto-1-propansulfonic acid (MPS) 2139 Estrone 3-sulfate CHO-OAT3 Astorga, 2011
Acetazolamide 816 Estrone 3-sulfate S2-OAT3 Hasannejad, 2004
Adipate 136 Estrone 3-sulfate HEK293-OAT3 Kaufhold, 2011
Alpha-ketoglutarate 92.8 Estrone 3-sulfate HEK293-OAT3 Kaufhold, 2011
Betamipron 48.3 Estrone 3-sulfate S2-OAT3 Takeda, 2001
Bumetanide 0.75 Estrone 3-sulfate S2-OAT3 Hasannejad, 2004
Bumetanide 7.8 Estrone 3-sulfate OAT3-expressing oocytes Elsby, 2011
Bumetanide 5.4 Methotrexate OAT3-expressing oocytes Elsby, 2011
Candesartan 0.3 Uric acid HEK293-OAT3 Sato, 2008
Cefadroxil 8620 Prostaglandin F2alpha S2-OAT3 Khamdang, 2003
Cefamandole 50 Prostaglandin F2alpha S2-OAT3 Khamdang, 2003
Cefazolin 550 Prostaglandin F2alpha S2-OAT3 Khamdang, 2003
Cefoperazone 1890 Prostaglandin F2alpha S2-OAT3 Khamdang, 2003
Cefotaxime 290 Prostaglandin F2alpha S2-OAT3 Khamdang, 2003
Ceftriaxone 4390 Prostaglandin F2alpha S2-OAT3 Khamdang, 2003
Cephaloridine 2460 Prostaglandin F2alpha S2-OAT3 Khamdang, 2003
Cephalothin 40 Prostaglandin F2alpha S2-OAT3 Khamdang, 2003
Chlorothiazide 65.3 Estrone 3-sulfate S2-OAT3 Hasannejad, 2004
Cilastatin 231 Estrone 3-sulfate S2-OAT3 Takeda, 2001
Cimetidine 79 Sitagliptin CHO-OAT3 Chu, 2007
Citrinin 15.4 Ochratoxin A S2-OAT2 Jung, 2001
Cyclothiazide 27.9 Estrone 3-sulfate S2-OAT3 Hasannejad, 2004
Diclofenac 7.78 Estrone 3-sulfate S2-OAT3 Khamdang, 2002
Ethacrynic acid 0.58 Estrone 3-sulfate S2-OAT3 Hasannejad, 2004
Fenofibric acid 2.2 Sitagliptin CHO-OAT3 Chu, 2007
Fluvastatin 5.79 Estrone 3-sulfate S2-OAT3 Takeda, 2004
Furosemide 7.31 Estrone 3-sulfate S2-OAT3 Hasannejad, 2004
Furosemide 1.7 Sitagliptin CHO-OAT3 Chu, 2007
Gemfibrozil 6.8 Pravastatin S2-OAT3 Nakagomi-Hagihara, 2007
Glutarate 78.5 Estrone 3-sulfate HEK293-OAT3 Kaufhold, 2011
Hydrochlorothiazide 942 Estrone 3-sulfate S2-OAT3 Hasannejad, 2004
Ibuprofen 6 Estrone 3-sulfate S2-OAT3 Khamdang, 2002
Ibuprofen 3.7 Sitagliptin CHO-OAT3 Chu, 2007
Indapamide 11 Sitagliptin CHO-OAT3 Chu, 2007
Indomethacin 0.61 Estrone 3-sulfate S2-OAT3 Khamdang, 2002
JBP485 185 160 Bestatin HEK293-OAT3 Zhu, 2012
Ketoprofen 5.98 Estrone 3-sulfate S2-OAT3 Khamdang, 2002
Losartan 1.6 Uric acid HEK293-OAT3 Sato, 2008
Mefenamic acid 0.78 Estrone 3-sulfate S2-OAT3 Khamdang, 2002
Methazolamide 97.5 Estrone 3-sulfate S2-OAT3 Hasannejad, 2004
Naproxen 4.67 Estrone 3-sulfate S2-OAT3 Khamdang, 2002
Novobiocin 4.99 4.77 Estrone 3-sulfate COS7-OAT3 Duan, 2009
Octanoate 8.6 Ochratoxin A S2-OAT2 Jung, 2001
Olmesartan 0.027 Uric acid HEK293-OAT3 Sato, 2008
Para-aminohippurate 19.6 Ochratoxin A S2-OAT2 Jung, 2001
Penicillin G 102 88 Bestatin HEK293-OAT3 Zhu, 2012
Phenacetin 19.4 Estrone 3-sulfate S2-OAT3 Khamdang, 2002
Pimelate 634 Estrone 3-sulfate HEK293-OAT3 Kaufhold, 2011
Piroxicam 2.52 Estrone 3-sulfate S2-OAT3 Khamdang, 2002
Piroxicam 4.88 Ochratoxin A S2-OAT2 Jung, 2001
Pratosartan 0.095 Uric acid HEK293-OAT3 Sato, 2008
Pravastatin 13.7 Estrone 3-sulfate S2-OAT3 Takeda, 2004
Probenecid* 3.1 Cimetidine CHO-OAT3 Chu, 2007
Probenecid 32 Dimesna HeLa-OAT3 Cutler, 2012
Probenecid* 9 Estrone 3-sulfate S2-OAT3 Takeda, 2001
Probenecid* 1.3 Fexofenadine HEK293-OAT3 Tahara, 2006
Probenecid* 4.41 Ochratoxin A S2-OAT3 Jung, 2001
Probenecid* 5.6 Sitagliptin CHO-OAT3 Chu, 2007
Quinapril 6.2 Sitagliptin CHO-OAT3 Chu, 2007
Simvastatin 32.3 Estrone 3-sulfate S2-OAT3 Takeda, 2004
Sitagliptin 160 Cimetidine CHO-OAT3 Chu, 2007
Suberate 232 Estrone 3-sulfate HEK293-OAT3 Kaufhold, 2011
Sulfasalazine 3 Methotrexate OAT3-expressing oocytes Elsby, 2011
Sulindac 3.62 Estrone 3-sulfate S2-OAT3 Khamdang, 2002
Telmisartan 1.6 Uric acid HEK293-OAT3 Sato, 2008
Trichloromethiazide 71.2 Estrone 3-sulfate S2-OAT3 Hasannejad, 2004
Valsartan 0.2 Uric acid HEK293-OAT3 Sato, 2008

ND = not determined


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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


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