PEPT1 Transporter Assay (SLC15A1)

PEPT1 is a high capacity, low affinity transporter that is expressed in the apical membrane of the intestines. It facilitates the absorption of substrates including small peptides and xenobiotics.

Prodrugs that are substrates of PEPT1 can have substantially increased oral bioavailability compared to the parent drug. Examples of such prodrugs include valganciclovir and valacyclovir, the valine esters ganciclovir and acyclovir.

Optivia offers PEPT1 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 PEPT1 inhibitors as well as Vmax and Km values for PEPT1 substrates.

PEPT1 Transporter Assay

Relevance – Intestinal uptake, prodrug strategy 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 – Gly-Sar
Subcellular Localization in Assay Model – Apical Inhibition Positive Control – Losartan