• OCT2

    EC50 values and relative Vmax for three different substrates using the SURFE²R N1.

  • OCT2

    Transient OCT2 currents recorded on the SURFE²R 96SE.

OCT2 - Organic Cation Transporter 2 - SLC22A2

Organic Cation Transporters (OCT) also known as Solute Carrier Family 22


The protein contains twelve putative transmembrane domains and is a plasma integral membrane protein.

OCT2: Background Information

SLC22A2, more commonly referred to as OCT2 (Organic Cation Transporter 2), is a renal uptake transporter that plays a key role in disposition and renal clearance of drugs and endogenous compounds. OCT2 substrate drugs have the potential for drug drug interactions with co-administered therapeutics that are inhibitors of this transporter. The FDA and EMA require in vitro testing for OCT2 liability with drug candidates that are eliminated at least in part via the kidneys.


Human Protein:
UniProt O15244

kidney, small intestine, lung, skin, placenta, brain and choroid plexus

Function/ Application:
In the basolateral membrane of the distal tubule in the kidney, OCT2 transporter mediates uptake from the blood to the proximal tubular cells during the renal secretion of organic cations. OCT2 transports many organic cations and play an important role on the pharmacological, pharmacokinetic and toxicological properties of therapeutics. OCT2 transports monoamine neurotransmitters, thereby participating in the regulation of interstitial and intracellular concentrations of monoamine neurotransmitters and cationic drugs.

OCT2 transporter contributes to renal drug uptake, clearance and transporter – mediated drug interactions.

choline, metformin, TEA

SURFE2R transporter assays

Recommended Reviews:
Koepsell, H. and H. Endou, The SLC22 drug transporter family. Pflugers Arch, 2004. 447(5): p. 666-76; Jonker, J.W. and A.H. Schinkel, Pharmacological and physiological functions of the polyspecific organic cation transporters: OCT1, 2, and 3 (SLC22A1-3). J Pharmacol Exp Ther, 2004. 308(1): p. 2-9; Koepsell, H., Polyspecific organic cation transporters: their functions and interactions with drugs. Trends Pharmacol Sci, 2004. 25(7): p. 375-81.

Data and Applications

Organic Cation Transporter 2 (OCT2) - Pharmacology


Icon N1 SURFE2R N1 data and applications:

EC50 values and relative Vmax for three different substrates are shown.

The IC50 value for Choline was determined as 4.6 mM, for TEA as 0.33 mM and for Metformin as 8.6 mM.

Organic Cation Transporter 2 (OCT2) - Application of Choline, TEA and Methformin


Icon 96SE   SURFE2R 96SE data and applications:

OCT2 transient currents are shown before and after the application of Choline, TEA and Methformin. A concentration-dependent activation of OCT2 could be obtained by all of the three compounds. Membranes without OCT2 (control membrane) were used as a negative control.


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