OCT1 Transporter Assay (SLC22A1)

The OCT1 transporter is an organic cation uptake transporter that is encoded by the SLC22A1 gene. OCT1 is expressed in liver hepatocytes on the basal-lateral side of the sinusoidal membrane. 

Optivia’s OCT1 Transporter Assay

Optivia offers OCT1 substrate and inhibition assays for transport in polarized mammalian cells. We offer a wide range of studies including single concentration screens up to full kinetic studies to determine the IC50 for OCT1 inhibitors as well as Vmax and Km values for OCT1 substrates.

OCT1 Transporter Assay

Relevance – EMA guidance; hepatic uptake Single or Multi-Transporter Model – Single
Transporter Type – Uptake Cell Model – MDCK-II
Assay Type – Intracellular accumulation Exactly Matched Control Cells – Yes
Species – Human Probe Substrate – Metformin or MPP+
Subcellular Localization in Assay Model – Basolateral Inhibition Positive Control – Quinidine

Clinical & Regulatory Relevance

OCT1 serves to bring substrates from the bloodstream into the liver, it can mediate the hepatic elimination of these compounds. Study of the OCT1 transporter is recommended in EMA guideline documents.

Applications & Therapeutic Areas

DDI/regulatory, toxicity/safety, pharmacokinetics, elimination, liver failure