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SLC47A1

Synonyms: FLJ10847, MATE1, MGC64822

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
Kidney* Mean across all PMT Samples   10.743
Liver* Mean across all PMT Samples   18.098
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
Acyclovir 2640 HEK293-MATE1 Tanihara, 2007
Cimetidine 170 HEK293-MATE1 Tanihara, 2007
Estrone 3-sulfate 470 HEK293-MATE1 Tanihara, 2007
Ganciclovir 5120 HEK293-MATE1 Tanihara, 2007
Guanidine 2100 HEK293-MATE1 Tanihara, 2007
Metformin 202 HeLa-MATE1 Meyer, 2010
Metformin 227 HEK293-MATE1 Chen, 2009
Metformin 780 HEK293-MATE1 Tanihara, 2007
N-methylpyridinium 16 HEK293-MATE1 Otsuka, 2005
N-methylpyridinium 100 HEK293-MATE1 Tanihara, 2007
Paraquat 169 HEK293-MATE1 Chen, 2009
Procainamide 1230 HEK293-MATE1 Tanihara, 2007
Tetraethylammonium 220 HEK293-MATE1 Otsuka, 2005
Tetraethylammonium 380 HEK293-MATE1 Xie, 2007
Topotecan 70 HEK293-MATE1 Tanihara, 2007

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
Amantadine 111.8 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Cetirizine 371.2 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Chloroquine 2.5 Metformin HEK293-MATE1 Muller, 2011
Chlorpheniramine 87.6 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Cimetidine 3.8 Metformin HEK293-MATE1 Ito, 2012
Cimetidine 1.1 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Desipramine 55.7 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Diltiazem 12.5 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Diphenhydramine 87 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Disopyramide 83.8 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
DX-619 0.82 Creatinine HEK293-MATE1 Imamura, 2011
Famotidine 0.6 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Imipramine 42 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Metformin 666.9 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Mitoxantrone 4.4 Metformin HeLa-MATE1 Meyer, 2010
Mitoxantrone 5.2 Tetraethylammonium HeLa-MATE1 Meyer, 2010
N-butylpyridinium chloride (NBuPy-Cl) 8.5 1-methyl-4-phenylpyridinium (MPP+) CHO-MATE1 Cheng, 2011
Pramipexole 141.4 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Procainamide 217 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Quinidine 29.2 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Ranitidine 18.9 Metformin HeLa-MATE1 Meyer, 2010
Ranitidine 17.5 Tetraethylammonium HeLa-MATE1 Meyer, 2010
Ranitidine 25.4 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Rapamycin 3.27 Metformin HeLa-MATE1 Meyer, 2010
Rapamycin 3.51 Tetraethylammonium HeLa-MATE1 Meyer, 2010
Ritonavir 15.4 Metformin HeLa-MATE1 Meyer, 2010
Ritonavir 13.9 Tetraethylammonium HeLa-MATE1 Meyer, 2010
Talipexole 66 Tetraethylammonium HEK293-MATE1 Tsuda, 2009
Verapamil 27.5 Tetraethylammonium HEK293-MATE1 Tsuda, 2009

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 OCTs/MATEs Cetirizine Pilsicainide 1.4 NS ND ND ND ND Tsuruoka, 2006 DDI 1
2 OCTs/MATEs Cimetidine Cephalexin NS NS 0.8 0.8 NS ND van, 1986 DDI 2
3 OCTs/MATEs Cimetidine Dofetilide 1.5 1.3 0.7 0.7 1.3 yes Abel, 2000 DDI 3
4 OCTs/MATEs Cimetidine Metformin 1.5 1.7 0.7 ND ND ND Somogyi, 1987 DDI 4
5 OCTs/MATEs Cimetidine Pilsicainide 1.3 NS 0.7 0.7 1.2 ND Shiga, 2000 DDI 5
6 OCTs/MATEs Cimetidine Pindolol (S-enantiomer) 1.4 1.3 0.7 ND NS ND Somogyi, 1992 DDI 6
7 OCTs/MATEs Cimetidine Procainamide 1.4 NS 0.6 ND 1.3 ND Somogyi, 1983 DDI 7
8 OCTs/MATEs Cimetidine Ranitidine 1.3 NS 0.7 ND 1.3 ND van, 1986 DDI 8
9 OCTs/MATEs Cimetidine Varenicline 1.3 ND 0.8 0.8 ND ND Feng, 2008 DDI 9
10 MATEs Pyrimethamine Metformin 1.4 1.4 0.6 ND ND ND Kusuhara, 2011 DDI 10

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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