SLC (Uptake) Transporters


OATPs, OCTs, OATs and MATEs are members of the solute-linked carrier superfamily and are expressed in many different epithelial membranes in the body. They function in intestinal absorption, blood-brain barrier penetration and excretion into the bile and urine. To evaluate if a test compound is a substrate of these transporters, the accumulation of the in transporter expressing cells and control cells is measured. Inhibition is evaluated by measuring the ability of the test compound to reduce the uptake of a probe substrate into the cells.
View schematics for liver, kidney, intestine and brain transporters


The two main organic anion transporting polypeptides, OATP1B1 (OATP-C, OAT2, LST-1, SLCO1B1) and OATP1B3 (OATP-8, SLCO1B3) are expressed in the liver and are involved in the distribution of drugs from the sinusoidal blood to hepatocytes. Pravastatin is a typical substrate and rifampin is a typical inhibitor of OATP transporters.


The two main members of this organic cation transporter family are OCT1 (SLCO22A1) and OCT2 (SLCO22A2). OCT is mainly expressed on the sinusoidal membrane of hepatocytes and transport compounds from the blood into the liver. OCT2 is expressed on the basolateral membrane of renal proximal tubules and transport compounds from the blood into proximal tubules. Metformin is a typical substrate and cimetidine is a typical inhibitor of OCT transporters.


Organic anion transporters, OAT1 (SLC22A6) and OAT3 (SLC22A8), are mainly expressed in the kidney and transport compounds into the proximal tubules for further excretion into urine. OAT inhibitors might inhibit the excretion of neurotransmitter metabolites and some drugs causing adverse effects. Acyclovir, cidovir and methotrexate are substrates of OAT1; furosemide, estrone sulfate and NSAIDs are substrates of OAT3. Probenecid and Novobiocin are inhibitors of both OAT1 and OAT3.


Multidrug and Toxin Extrusion 1 (MATE1/SLC47A1) and Multidrug and Toxin Extrusion 2K (MATE2K/SLC47A2) are transporters that are expressed in the renal proximal tubule and function in the secretion of cations into the urine. MATE1 is also expressed at the canalicular membrane of hepatocytes where it is involved in biliary excretion. MATE transporters overlap in substrate specificity and work in tandem with OCT transporters. Metformin and N-methylpyridinium are common MATE substrates and cimetidine and pyrimethamne are common MATE inhibitors.

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Uptake Transporter Assay Design