hOAT1 (SLC22A6)

The human organic anion transporter 1 (OAT1; SLC22A6) is highly expressed at the basolateral membrane of proximal tubule cells in human kidneys. There OAT1 mediates the transport of numerous endogenous and exogenous compounds like antibiotics, diuretics, NSAID (non-steroidal anti-inflammatory drugs), antivirals, cytostatics and toxins. OAT1 facilitate the first step uptake at basolateral membrane of proximal tubule cells for renal secretion of a huge number of substrates. Therefore, the regulatory agencies decided that drugs eliminated significantly via the kidney have to be tested as potential inhibitors (substrates) for hOAT1.

Main localization:
Transporter assay:
Uptake transporter assay (potential inhibitors or substrates)
Probe substrates:
p-Aminohippuric acid (PAH)
Probe inhibitors:
Probenecid, glibenclamide
Regulatory relevance:
FDA and EMA guidance
Important interacting drugs:
Adefovir, acyclovir, methotrexate, ochratoxin A, olmesartan, probenecid, bumetanide, diclofenac, fluvastatin, furosemide, ibuprofen
From other species:
rOat1, mOat1

Inhibition of hOAT1 mediated PAH uptake by different drugs (100 µM)
Home | Services | Drug Transporter Assays | Drug Transporter | About us | News and Events | Contact | Imprint | Privacy Policy

PortaCellTec Biosciences GmbH • Science Park Va • Marie-Curie-Straße 8 • 37079 Göttingen • Germany • T. 0049 551 309 66440 • F. 0049 551 309 66442 •
info@portacelltec.de • © PortaCellTec Biosciences 2021